Page last updated: 2024-12-08

tesaglitazar

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Description

tesaglitazar: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID208901
CHEMBL ID282686
SCHEMBL ID16594
MeSH IDM0486171

Synonyms (73)

Synonym
AC-6748
(s)-2-ethoxy-3-(4-((4-(methylsulfonyloxy)phenethyl)oxy)phenyl)propanoic acid
2-ethoxy-3-(4-((4-(methylsulfonyloxy)phenethyl)oxy)phenyl)propanoic acid
(s)-2-ethoxy-3-(4-(2-(4-methylsulphonyloxyphenyl)ethoxy)phenyl)propanoic acid
ar-h-039242
br-44608 ,
CHEMBL282686
az-242
ar-h039242xx
tesaglitazar
galida
(2s)-2-ethoxy-3-[4-(2-{4-[(methylsulfonyl)oxy]phenyl}ethoxy)phenyl]propanoic acid
(2s)-2-ethoxy-3-(4-{2-[4-(methanesulfonyloxy)phenyl]ethoxy}phenyl)propanoic acid
bdbm28798
1I7G
1I7I
az 242
251565-85-2
tesaglitazar (jan/usan/inn)
D01274
DB07399
(2s)-2-ethoxy-3-[4-[2-(4-methylsulfonyloxyphenyl)ethoxy]phenyl]propanoic acid
NCGC00182082-02
(2s)-2-ethoxy-3-(4-(2-(4-((methylsulfonyl)oxy)phenyl)ethoxy)phenyl)propionic acid
(2s)-2-ethoxy-3-(4-(2-(4-((methylsulfonyl)oxy)phenyl)ethoxy)phenyl)propanoic acid
tesaglitazar [usan:inn]
6734037o3l ,
benzenepropanoic acid, alpha-ethoxy-4-(2-(4-((methylsulfonyl)oxy)phenyl)ethoxy)-, (alphas)-
unii-6734037o3l
benzenepropanoic acid, a-ethoxy-4-[2-[4-[(methylsulfonyl)oxy]phenyl]ethoxy]-, (as)-
(s)-2-ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propionic acid
(s)-2-ethoxy-3-(4-[2-(4-methanesulfonyloxy-phenyl)-ethoxy]-phenyl)-propionic acid
dtxsid4048773 ,
(s)-2-ethoxy-3-(4-(4-((methylsulfonyl)oxy)phenethoxy)phenyl)propanoic acid
A817671
smr003500714
MLS004774044
(s)-2-ethoxy-3-{4-[2-(4-methanesulfonyloxy-phenyl)-ethoxy]-phenyl}-propionic acid
AKOS015920483
tesaglitazar [usan]
(2s)-2-ethoxy-3-[4-[2-[4-[(methylsulfonyl)oxy]phenyl]ethoxy]phenyl]propanoic acid
(s)-2-ethoxy-3-(4-(2-(4-methylsulfonyloxyphenyl)ethoxy)phenyl)propanoic acid
tesaglitazar [jan]
tesaglitazar [who-dd]
benzenepropanoic acid,.alpha.-ethoxy-4-(2-(4-((methylsulfonyl)oxy)phenyl)ethoxy) ,(.alpha.s)-
tesaglitazar [inn]
tesaglitazar [mi]
(s)-2-ethoxy-3-{4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl}propionic acid
c20h24o7s
SCHEMBL16594
(s)-2-ethoxy-3-(4-(4-(methylsulfonyloxy)phenethoxy)phenyl)propanoic acid
(s)-2-ethoxy-3-[4-(2-{4-methanesulfonyloxyphenyl}ethoxy)phenyl]propanoic acid
CXGTZJYQWSUFET-IBGZPJMESA-N
(s)-2-ethoxy-3-[4-(2-{4-methanesulfonyloxyphenyl} ethoxy)phenyl]propanoic acid
(s)-2-ethoxy-3-[4-(2-{4-methanesulfonyloxyphenyl}-ethoxy)phenyl]propanoic acid
(s)-2-ethoxy-3-[4-(2-{4-methanesulfonyloxyphenyl}ethoxy) phenyl]propanoic acid
(s)-2-ethoxy-3-[4-[[4-(methylsulphonyloxy)phenethyl]oxy]phenyl]propanoic acid
T3497
(s)-2-ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic acid
mfcd07784004
tesaglitazar, >=98% (hplc)
J-015842
HY-17444
DB06536
AS-35360
tesaglitizar
(s)-2-ethoxy-3-[4-[4-[(methylsulfonyl)oxy]phenethoxy]phenyl]propanoic acid
Q7705411
CS-0008240
(s)-2-ethoxy-3-(4-(4-((methylsulfonyl)-oxy)phenethoxy)phenyl)propanoic acid
(s)-2-ethoxy-3-(4-(4-((methylsulfonyl)oxy)phenethoxy)phenyl)propanoicacid
(s)-2-ethoxy-3-[4-[2-(4-methanesulf onyloxyphenyl)ethoxy]phenyl]propanoic acid
benzenepropanoic acid, alpha-ethoxy-4-[2-[4-[(methylsulfonyl)oxy]phenyl]ethoxy]-, (alphas)-

Research Excerpts

Overview

Tesaglitazar is a dual-acting PPARalpha/gamma agonist currently being investigated in phase III clinical trials. It is being investigated as an alternative treatment for insulin resistance and the characteristic dyslypidemia of type 2 diabetes.

ExcerptReferenceRelevance
"Tesaglitazar is a dual-acting PPARalpha/gamma agonist currently being investigated in phase III clinical trials as an alternative treatment for insulin resistance and the characteristic dyslypidemia of type 2 diabetes."( Tesaglitazar: a promising approach in type 2 diabetes.
Cox, SL, 2006
)
2.5
"Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist in development to treat lipid and glucose abnormalities associated with type 2 diabetes. "( Food does not affect the pharmacokinetics of tesaglitazar, a novel dual peroxisome proliferator-activated receptor alpha/gamma agonist.
Halldórsdóttir, S; Johansson, S; Ohman, KP; Samuelsson, S; Stenhoff, H, 2006
)
2.04

Effects

Tesaglitazar has anti-atherosclerotic effects in the mouse model that go beyond plasma cholesterol lowering, possibly caused by a combination of altered lipoprotein profiles and anti-inflammatory vascular effects.

ExcerptReferenceRelevance
"Tesaglitazar has anti-inflammatory effects in the diabetic LDLr-/- mice. "( [Peroxisome proliferator-activated receptor α/γ agonist tesaglitazar stabilizes atherosclerotic plaque in diabetic low density lipoprotein receptor knockout mice].
Che, WL; Hou, L; Li, WM; Li, XK; Wei, YD; Xu, YW; Zhang, BC, 2013
)
2.08
"Tesaglitazar has anti-atherosclerotic effects in the mouse model that go beyond plasma cholesterol lowering, possibly caused by a combination of altered lipoprotein profiles and anti-inflammatory vascular effects."( Dual PPARalpha/gamma agonist tesaglitazar reduces atherosclerosis in insulin-resistant and hypercholesterolemic ApoE*3Leiden mice.
Boesten, LS; Camejo, G; Emeis, JJ; Havekes, LM; Jukema, JW; Kooistra, T; Lundholm, E; van Vlijmen, BJ; Zadelaar, AS, 2006
)
2.07

Treatment

Tesaglitazar treatment in OZR significantly reduced nonfasting glucose, C-reactive protein levels and improved dyslipidemia. Mice treated with tesag litazar-containing chow or high fat diet developed cardiac dysfunction despite lower plasma triglycerides and glucose levels.

ExcerptReferenceRelevance
"Tesaglitazar treatment in OZR significantly reduced nonfasting glucose, C-reactive protein levels and improved dyslipidemia."( Tesaglitazar, a dual peroxisome proliferator-activated receptor agonist (PPAR alpha/gamma), improves metabolic abnormalities and reduces renal injury in obese Zucker rats.
Aguilar, E; Asghar, A; Ebenezer, P; Ferder, L; Francis, J; Hu, X; Isidro-Carrión, AA; Liao, J; Reisin, E; Soltani, Z; Zhang, R, 2010
)
2.52
"All tesaglitazar-treated patients had a reduction in glomerular filtration rate, and available demographic variables could not explain differences in response."( Pharmacokinetic-pharmacodynamic assessment of the interrelationships between tesaglitazar exposure and renal function in patients with type 2 diabetes mellitus.
Hamrén, B; Karlsson, MO; Ohman, KP; Svensson, MK, 2012
)
1.09
"Mice treated with tesaglitazar-containing chow or high fat diet developed cardiac dysfunction despite lower plasma triglycerides and glucose levels."( Dual peroxisome-proliferator-activated-receptor-α/γ activation inhibits SIRT1-PGC1α axis and causes cardiac dysfunction.
Area-Gomez, E; Chin, A; Civelek, M; Drosatos, K; Goldberg, IJ; Kalliora, C; Kyriazis, ID; Lieu, MJ; Madesh, M; Mizushima, W; Oka, SI; Pol, CJ; Sadoshima, J; Scerbo, D; Schulze, PC; Tian, Y; Yue, Y, 2019
)
0.84
"Treatment with tesaglitazar significantly reduced plasma triglycerides, total cholesterol, CETP mass and CETP activity, and increased high-density lipoprotein-cholesterol. "( The dual PPARalpha/gamma agonist tesaglitazar blocks progression of pre-existing atherosclerosis in APOE*3Leiden.CETP transgenic mice.
Camejo, G; Havekes, LM; Jukema, JW; Lundholm, E; Princen, HM; Rensen, PC; van der Hoorn, JW, 2009
)
0.99
"Treatment with tesaglitazar resulted in changes typical for exaggerated PPARα pharmacology in rodents, such as hepatocellular hypertrophy and hepatocellular carcinoma, but not an increased frequency of hemangiosarcomas."( Tesaglitazar, a dual PPAR-α/γ agonist, hamster carcinogenicity, investigative animal and clinical studies.
Berg, AL; Blomgren, B; Evans, J; Hellmold, H; Lindblom, P; Lundgren, H; Marcusson-Ståhl, M; Öhman, P; Sjögren, N; Skånberg, I; Tugwood, J; Westerberg, R; Zhang, H, 2012
)
2.16
"Treatment with tesaglitazar lowered fasting plasma glucose, improved glucose tolerance, substantially reduced fasting and postload insulin levels, and markedly lowered fasting TG and improved lipid tolerance."( Tesaglitazar, a dual PPAR{alpha}/{gamma} agonist, ameliorates glucose and lipid intolerance in obese Zucker rats.
Camejo, G; Hultstrand, T; Jacinto, S; Ljung, B; Oakes, ND; Thalén, P; Wallin, B, 2005
)
2.11
"Treatment with tesaglitazar was associated with reduced plasma insulin and total triglyceride levels and increased plasma adiponectin levels."( Peroxisome proliferator activated receptor alpha/gamma dual agonist tesaglitazar attenuates diabetic nephropathy in db/db mice.
Breyer, MD; Cha, DR; Fang, X; Guan, Y; Han, JY; Su, D; Wu, J; Yu, B; Zhang, X; Zhang, Y, 2007
)
0.91

Toxicity

ExcerptReferenceRelevance
"In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, novel thiophene substituted oxazole containing α-alkoxy-phenylpropanoic acid derivatives are designed as highly potent PPARα/γ dual agonists."( Revisiting glitazars: thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents.
Basu, S; Giri, S; Gite, A; Godha, A; Goswami, A; Jain, M; Patel, P; Pingali, H; Raval, P; Raval, S; Shah, M; Suthar, D, 2011
)
0.37

Pharmacokinetics

The elimination half-life of radioactivity and tesaglitazar was approximately 45 h. A mechanistic understanding of the pharmacokinetic properties of tesglitazar and its metabolite is needed.

ExcerptReferenceRelevance
" Blood samples were taken to assess pharmacokinetic variables."( Food does not affect the pharmacokinetics of tesaglitazar, a novel dual peroxisome proliferator-activated receptor alpha/gamma agonist.
Halldórsdóttir, S; Johansson, S; Ohman, KP; Samuelsson, S; Stenhoff, H, 2006
)
0.59
" A mechanistic understanding of the pharmacokinetic properties of tesaglitazar and its metabolite."( Mechanistic modelling of tesaglitazar pharmacokinetic data in subjects with various degrees of renal function--evidence of interconversion.
Ericsson, H; Hamrén, B; Karlsson, MO; Samuelsson, O, 2008
)
0.89
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35

Bioavailability

ExcerptReferenceRelevance
" Tesaglitazar absorption was rapid, with maximum plasma concentration (C(max)) at approximately 1 h postdose, and the absolute bioavailability was approximately 100%, suggesting no, or negligible, first-pass metabolism."( Pharmacokinetics and metabolism of tesaglitazar, a novel dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist, after a single oral and intravenous dose in humans.
Bergstrand, S; Elebring, M; Ericsson, H; Fryklund, L; Hamrén, B; Heijer, M; Ohman, KP, 2004
)
1.51
" c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid 13c exhibited potent hypoglycemic and lipid lowering activity with high oral bioavailability in animal models."( Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
Basu, S; Giri, S; Godha, A; Goel, A; Goswami, A; Jain, M; Makadia, P; Patel, H; Patel, M; Patel, P; Patil, P; Pingali, H; Shah, S; Zaware, P, 2008
)
0.35
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
0.36

Dosage Studied

The Glucose and Lipid Assessment in Diabetes (GLAD) trial examined the dose-response relationship of the dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist tesaglitazar.

ExcerptRelevanceReference
"The Glucose and Lipid Assessment in Diabetes (GLAD) trial examined the dose-response relationship of the dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist tesaglitazar in type 2 diabetic patients."( Effect of tesaglitazar, a dual PPAR alpha/gamma agonist, on glucose and lipid abnormalities in patients with type 2 diabetes: a 12-week dose-ranging trial.
Anzalone, D; Goldstein, BJ; Ohman, KP; Rosenstock, J; Tou, C, 2006
)
0.93
" A possible modelling framework to evaluate interconversion without dosing of the metabolite based on the simultaneous analysis of plasma and urine data from a group of subjects with varying renal function."( Mechanistic modelling of tesaglitazar pharmacokinetic data in subjects with various degrees of renal function--evidence of interconversion.
Ericsson, H; Hamrén, B; Karlsson, MO; Samuelsson, O, 2008
)
0.65
"Data were from a 6-week study in subjects with renal insufficiency and matched controls undergoing repeated oral dosing with tesaglitazar (n = 41)."( Mechanistic modelling of tesaglitazar pharmacokinetic data in subjects with various degrees of renal function--evidence of interconversion.
Ericsson, H; Hamrén, B; Karlsson, MO; Samuelsson, O, 2008
)
0.86
" The model and data give insight into the likely mechanism (interconversion) of the increased tesaglitazar exposure in renally impaired subjects, and separate elimination and interconversion processes without dosing of the metabolite."( Mechanistic modelling of tesaglitazar pharmacokinetic data in subjects with various degrees of renal function--evidence of interconversion.
Ericsson, H; Hamrén, B; Karlsson, MO; Samuelsson, O, 2008
)
0.87
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHAHomo sapiens (human)IC50 (µMol)0.60000.20000.60001.0000AID977608
Chain A, PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMAHomo sapiens (human)IC50 (µMol)0.60000.20000.60001.0000AID977608
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)IC50 (µMol)0.35000.00501.205110.0000AID156959
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Ki0.01800.00000.37905.6000AID314545
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)Ki0.20000.20000.20000.2000AID238821
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)IC50 (µMol)3.80000.00050.82696.3100AID156285
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)Ki1.00000.00011.01894.5000AID238820
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Peroxisome proliferator-activated receptor alphaMus musculus (house mouse)EC50 (µMol)1.70000.00021.397110.0000AID1467413
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC50 (µMol)2.35940.00000.992210.0000AID1467409; AID156797; AID1798927; AID289933; AID348511; AID387492; AID391553; AID717061
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)EC50 (µMol)0.25000.00031.654210.0000AID1467414; AID240316
Cannabinoid receptor 2Mus musculus (house mouse)EC50 (µMol)0.70400.00730.15460.7040AID391553
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)EC50 (µMol)3.21160.00061.607410.0000AID1467407; AID155986; AID1798927; AID240310; AID289934; AID314546; AID314548; AID348510; AID387491; AID391555; AID717062
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (107)

Processvia Protein(s)Taxonomy
negative regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of cholesterol effluxPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
long-chain fatty acid transportPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of osteoblast differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of smooth muscle cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of receptor signaling pathway via STATPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of low-density lipoprotein receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of signaling receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of BMP signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of MAP kinase activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of adiponectin secretionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cardiac muscle hypertrophy in response to stressPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of connective tissue replacement involved in inflammatory response wound healingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
placenta developmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
signal transductionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
G protein-coupled receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
response to nutrientPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of blood pressurePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cholesterol storagePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of lipid storagePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of sequestering of triglyceridePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of angiogenesisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
monocyte differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
BMP signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
epithelial cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to insulin stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
response to lipidPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
peroxisome proliferator activated receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
glucose homeostasisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of circadian rhythmPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
mRNA transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipoprotein transportPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of blood vessel endothelial cell migrationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
innate immune responsePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell fate commitmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of fat cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
retinoic acid receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell maturationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
rhythmic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
white fat cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipid homeostasisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of type II interferon-mediated signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of SMAD protein signal transductionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of cholesterol transporter activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to low-density lipoprotein particle stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to hypoxiaPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of mitochondrial fissionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of cellular response to insulin stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of extracellular matrix assemblyPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cellular response to transforming growth factor beta stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of adipose tissue developmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of vascular associated smooth muscle cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell apoptotic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of vascular endothelial cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of fatty acid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
fatty acid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of inflammatory responsePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
hormone-mediated signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cytokine production involved in inflammatory responsePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of reactive oxygen species biosynthetic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of hepatocyte apoptotic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of signaling receptor activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of ATP biosynthetic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of transformation of host cell by virusPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
response to hypoxiaPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
gluconeogenesisPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
heart developmentPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
response to nutrientPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
epidermis developmentPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
cellular response to starvationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
regulation of cellular ketone metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of cholesterol storagePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of sequestering of triglyceridePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
regulation of fatty acid metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
intracellular receptor signaling pathwayPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of fatty acid beta-oxidationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of appetitePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
response to insulinPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
circadian regulation of gene expressionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
behavioral response to nicotinePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
wound healingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
lipoprotein metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
regulation of circadian rhythmPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
steroid hormone mediated signaling pathwayPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
response to ethanolPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of gluconeogenesisPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of blood pressurePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of glycolytic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nitric oxide metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of fatty acid oxidationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of lipid biosynthetic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of inflammatory responsePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of cell growth involved in cardiac muscle cell developmentPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
enamel mineralizationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
cellular response to fructose stimulusPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of leukocyte cell-cell adhesionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
regulation of fatty acid transportPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
hormone-mediated signaling pathwayPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
fatty acid metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of fatty acid metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
cell differentiationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (40)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
transcription coregulator bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleic acid bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
chromatin bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
double-stranded DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nuclear receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
prostaglandin receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
zinc ion bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
enzyme bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
peptide bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
identical protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
sequence-specific DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nuclear retinoid X receptor bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
arachidonic acid bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA binding domain bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
LBD domain bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
alpha-actinin bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
R-SMAD bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
E-box bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
STAT family protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription activator activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
transcription coactivator bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription factor activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nuclear steroid receptor activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nuclear receptor activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
protein bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
zinc ion bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
lipid bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
phosphatase bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
protein domain specific bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
mitogen-activated protein kinase kinase kinase bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
ubiquitin conjugating enzyme bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
sequence-specific DNA bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
protein-containing complex bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
NFAT protein bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
MDM2/MDM4 family protein bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription factor bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
nucleoplasmPeroxisome proliferator-activated receptor alphaMus musculus (house mouse)
nucleusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleoplasmPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cytosolPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
intracellular membrane-bounded organellePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
RNA polymerase II transcription regulator complexPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
chromatinPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
receptor complexPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleoplasmPeroxisome proliferator-activated receptor gammaMus musculus (house mouse)
nucleusPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nucleoplasmPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
chromatinPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (95)

Assay IDTitleYearJournalArticle
AID552406Antihyperglycemic activity in db/db mouse assessed as reduction of serum glucose level at 3 mg/kg, po qd for 14 days relative to control2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists.
AID314545Displacement of [3H]Rosiglitazone from human PPARgamma2008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
AID314548Agonist activity at human PPARalpha at 100 uM by GAL4 transactivation assay relative to WY 14,6432008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID387491Agonist activity at human PPARalpha expressed in african green monkey CV-1 by co-transfected with GAL4 by by dual-glo luciferase reporter gene assay2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID289934Agonist activity at human PPARalpha in HepG2 cells by PPAR-GAL4 transactivation assay2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
AID424500Metabolic stability in rat hepatocyte microsomes2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1665654Renal toxicity in C57BL/6 mouse assessed effect on Fasn gene expression in kidney at 9.14 umol/kg, ip administered once daily for 7 days by Trizol reagent based RT-qPCR analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators.
AID365534Hypoglycemic activity in db/db mouse assessed as reduction in plasma glucose level at 3 mg/kg/day, po for 6 days2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID314547Agonist activity at human PPARgamma by GAL4 transactivation assay2008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
AID289933Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
AID317705Inhibition of PPARalpha at 50 uM2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.
AID365544Hypoglycemic activity in Zucker diabetic fa/fa rat assessed as improvement in glucose AUC at 3 mg/kg/day, po for 14 days2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID1665653In vivo agonist activity at PPAR in C57BL/6 mouse assessed upregulation of Pgc1-alpha gene expression at 9.14 umol/kg, ip administered once daily for 7 days by Trizol reagent based RT-qPCR analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID156285Receptor binding affinity to human Peroxisome proliferator activated receptor alpha against [3H]-NNC 0061-4655 radioligand2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
AID717062Agonist activity at GAL4-fused PPARalpha assessed as transcriptional activity by cell based assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).
AID1467414Agonist activity at 3' GAL4 DNA binding domain fused mouse PPARgamma LBD expressed in U-2 OS cells after 40 hrs by luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID391553Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
AID1698002Intrinsic clearance in cryopreserved human hepatocytes at 1 uM measured up to 120 mins by LC-MS/MS analysis
AID1467408Agonist activity at GAL4N fused human PPARalpha LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay relative to GW76472017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID348516Hypolipidemic activity in high cholesterol fed Sprague-Dawley rat assessed as reduction of LDL-C level at 3 mg/kg/day for 6 days relative to control2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID289945Decrease in plasma glucose level in db/db mouse at 1 mg/kg, po2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
AID314546Agonist activity at human PPARalpha by GAL4 transactivation assay2008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1467410Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay relative to rosiglitazone2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID1467407Agonist activity at GAL4N fused human PPARalpha LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID348509Reduction of triglyceride level in Swiss albino mouse serum at 10 mg/kg/day, po for 6 days relative to control2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID289948Decrease in plasma triglyceride level in db/db mouse at 1 mg/kg, po2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
AID365540Hypolipidemic activity in Zucker diabetic fa/fa rat assessed as reduction in total cholesterol level at 3 mg/kg/day, po for 14 days2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID314549Agonist activity at human PPARgamma at 1 uM by GAL4 transactivation assay relative to rosiglitazone2008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part I: synthesis and pharmacological evaluation.
AID610315Antihyperglycemic activity in db/db mouse assessed as reduction in glucose level at 3 mg/kg/day, po administered for 6 days relative to control2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
Revisiting glitazars: thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents.
AID1698006Ratio of drug level in cynomolgus monkey blood to plasma administered through iv dosing by LC-MS/MS analysis
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID391554Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay relative to rosiglitazone2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1468730Toxicity in Sprague-Dawley rat assessed as reduction in hematocrit level at 10 mg/kg for 4 weeks2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID424498Absorption in human Caco-2 cells2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID387492Agonist activity at human PPARgamma expressed in african green monkey CV-1 co-transfected with GAL4 by by dual-glo luciferase reporter gene assay2008Bioorganic & medicinal chemistry letters, Sep-15, Volume: 18, Issue:18
Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID348515Hypolipidemic activity in high cholesterol fed Sprague-Dawley rat assessed as reduction of total cholesterol level at 3 mg/kg/day for 6 days relative to control2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID365538Hypolipidemic activity in Zucker diabetic fa/fa rat assessed as reduction in triglyceride level at 3 mg/kg/day, po for 14 days2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID424502Glucose lowering effect in po dosed C57BL/6J ob/ob mouse assessed as glycemia relative to untreated control2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID348511Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID348512Hypolipidemic activity in db/db mouse assessed as reduction of triglyceride level at 3 mg/kg/day for 6 days relative to control2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID552407Antihyperlipidemic activity in db/db mouse assessed as reduction of serum triglyceride level at 3 mg/kg, po qd for 14 days relative to control2011Bioorganic & medicinal chemistry, Jan-15, Volume: 19, Issue:2
Effect of structurally constrained oxime-ether linker on PPAR subtype selectivity: Discovery of a novel and potent series of PPAR-pan agonists.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1697999Dissociation constant, acidic pKa of compound measured up to 18 mins by capillary electrophoresis
AID391556Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay relative to gemfibrozil2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
AID156797Agonistic activity for human Peroxisome proliferator activated receptor gamma2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1467413Agonist activity at 3' GAL4 DNA binding domain fused mouse PPARalpha LBD expressed in U-2 OS cells after 40 hrs by luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID424503Glucose lowering effect in po dosed C57BL/6J ob/ob mouse assessed as insulin level relative to untreated control2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID1698009Hepatic clearance in cynomolgus monkey at < 1 mg/kg, iv administered as cassette dosing
AID1467420Agonist activity at GAL4N fused human PPARdelta LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc at 50 uM after 24 hrs by luciferase reporter gene assay relative to control2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID348517Hypolipidemic activity in high cholesterol fed Sprague-Dawley rat assessed as effect on HDL-C level at 3 mg/kg/day for 6 days relative to control2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID348510Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID348514Hypolipidemic activity in high cholesterol fed Sprague-Dawley rat assessed as reduction of triglyceride level at 3 mg/kg/day for 6 days relative to control2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID365536Hypolipidemic activity in db/db mouse assessed as reduction in triglyceride level at 3 mg/kg/day, po for 6 days2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID717061Agonist activity at GAL4-fused PPARgamma assessed as transcriptional activity by cell based assay2012Bioorganic & medicinal chemistry letters, Dec-01, Volume: 22, Issue:23
Design, synthesis and evaluation of novel zwitterionic compounds as PPARα/γ dual agonists (1).
AID1698007Ratio of drug level in human blood to plasma administered through iv dosing by LC-MS/MS analysis
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID391555Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Design, synthesis, and biological evaluation of novel constrained meta-substituted phenyl propanoic acids as peroxisome proliferator-activated receptor alpha and gamma dual agonists.
AID317706Inhibition of PPARgamma at 1 uM2008Bioorganic & medicinal chemistry, Mar-01, Volume: 16, Issue:5
Omega-(2-Naphthyloxy) amino alkanes as a novel class of anti-hyperglycemic and lipid lowering agents.
AID155986Agonistic activity for Peroxisome proliferator activated receptor alpha2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
AID424499Metabolic stability in human hepatocyte microsomes2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID1468736Toxicity in Sprague-Dawley rat assessed as increase in heart weight at 10 mg/kg for 6 weeks2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1698011Fraction unbound in human plasma
AID1665619AUC (0.5 to 6 hrs) in C57BL/6 mouse serum at 9.14 umol/kg, ip by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators.
AID156959Receptor binding affinity to human Peroxisome proliferator activated receptor gamma against [3H]ragalitazar radioligand2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
AID1698004Fraction unbound in cynomolgus monkey plasma
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1468733Toxicity in Sprague-Dawley rat assessed as increase in plasma volume at 10 mg/kg for 4 weeks by evans blue dye based assay2018Journal of medicinal chemistry, 03-22, Volume: 61, Issue:6
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
AID1665608AUC (0.5 to 6 hrs) in C57BL/6 mouse brain at 9.14 umol/kg, ip by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators.
AID1698010Hepatic clearance in human administered through iv dosing
AID1665630Brain to serum concentration ratio, Kp of the compound in C57BL/6 mouse at 9.14 umol/kg, ip by LC-MS/MS analysis2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators.
AID240316Effective concentration against murine peroxisome proliferator activated receptor gamma in Gal4 transactivation assay2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
AID238820Binding affinity for human peroxisome proliferator activated receptor alpha2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
AID1467409Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Switching subtype-selectivity: Fragment replacement strategy affords novel class of peroxisome proliferator-activated receptor α/δ (PPARα/δ) dual agonists.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID424504Effect on bodyweight in po dosed C57BL/6J ob/ob mouse assessed as body weight gain relative to untreated control2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID348513Hypoglycemic activity in db/db mouse assessed as reduction of plasma glucose level at 3 mg/kg/day for 6 days relative to control2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent.
AID240310Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
AID424501Lipid lowering effect in po dosed C57BL/6J ob/ob mouse assessed as triglyceride level relative to untreated control2009Bioorganic & medicinal chemistry letters, May-15, Volume: 19, Issue:10
4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPARalpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations.
AID365542Insulin sensitizing activity in Zucker diabetic fa/fa rat assessed as reduction in fasted insulin level at 3 mg/kg/day, po for 14 days2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
AID238821Binding affinity for murine peroxisome proliferator activated receptor gamma2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
AID1698001Lipophilicity, log D of the compound at pH 7.4 by by shake flask method
AID1811Experimentally measured binding affinity data derived from PDB2001Structure (London, England : 1993), Aug, Volume: 9, Issue:8
Structure of the PPARalpha and -gamma ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2001Structure (London, England : 1993), Aug, Volume: 9, Issue:8
Structure of the PPARalpha and -gamma ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family.
AID1798927Cell-Based Transcription Assay from Article 10.1016/j.bmcl.2006.11.050: \\Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.\\2007Bioorganic & medicinal chemistry letters, Feb-15, Volume: 17, Issue:4
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (74)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's44 (59.46)29.6817
2010's22 (29.73)24.3611
2020's8 (10.81)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.78

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index27.78 (24.57)
Research Supply Index4.48 (2.92)
Research Growth Index4.41 (4.65)
Search Engine Demand Index32.40 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.78)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials13 (17.57%)5.53%
Reviews7 (9.46%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other54 (72.97%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]