Page last updated: 2024-11-08

drf 2725

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

ragaglitazar: a phenoxazine analogue of phenyl propanoic acid; Ragaglitazar is a coligand of PPARalpha and PPARgamma [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID447458
CHEMBL ID24038
SCHEMBL ID4822459
MeSH IDM0395629

Synonyms (26)

Synonym
gtpl2664
DRF ,
(2s)-2-ethoxy-3-{4-[2-(10h-phenoxazin-10-yl)ethoxy]phenyl}propanoic acid
nnc-61-0029
(-)-drf-2725
drf-2725
ragaglitazar
1NYX
CHEMBL24038 ,
(2s)-2-ethoxy-3-[4-(2-phenoxazin-10-ylethoxy)phenyl]propanoic acid
DB07675
2-ethoxy-3-[4-(2-phenoxazin-10-yl-ethoxy)-phenyl]-propionic acid
bdbm50109551
2-ethoxy-3-[4-(2-phenoxazin-10-yl-ethoxy)-phenyl]-propionic acid(-) drf 2725
(s)-2-ethoxy-3-[4-(2-phenoxazin-10-yl-ethoxy)-phenyl]-propionic acid
222834-30-2
nnc 61-0029
drf2725
WMUIIGVAWPWQAW-DEOSSOPVSA-N
SCHEMBL4822459
Q27088511
drf 2725; nn 622
CS-0006329
HY-16421
benzenepropanoic acid, alpha-ethoxy-4-[2-(10h-phenoxazin-10-yl)ethoxy]-, (alphas)-
AKOS040749270

Research Excerpts

Overview

DRF 2725 (6) is a phenoxazine analogue of phenyl propanoic acid.

ExcerptReferenceRelevance
"(-)DRF 2725 (6) is a phenoxazine analogue of phenyl propanoic acid. "( (-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
Bajji, AC; Chakrabarti, R; Juluri, S; Kalchar, S; Lohray, BB; Lohray, VB; Mamidi, NV; Misra, P; Padakanti, S; Poondra, RR; Rajagopalan, R; Vikramadithyan, RK, 2001
)
1.17

Toxicity

ExcerptReferenceRelevance
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36

Pharmacokinetics

ExcerptReferenceRelevance
" The application of the assay to a pharmacokinetic study in rats is described."( Quantitative determination of ragaglitazar in rat plasma by HPLC: validation and application in pharmacokinetic study.
Kota, J; Mamidi, RN; Mullangi, R; Rajagopalan, R, 2002
)
0.31
"7 h), with mean AUC0-24 h and Cmax proportional to dose after single and multiple dosing; t1/2 was 80 hours following a single dose and 104 hours in healthy subjects and 122 hours in patients after multiple dosing."( Ragaglitazar: the pharmacokinetics, pharmacodynamics, and tolerability of a novel dual PPAR alpha and gamma agonist in healthy subjects and patients with type 2 diabetes.
Drake, PG; Edsberg, B; Müller, M; Nielsen, KK; Pabst, G; Skrumsager, BK, 2003
)
0.32
" Plasma concentration versus time data were generated following oral and intravenous dosing and pharmacokinetic analysis was performed using non-compartmental analysis."( Intravenous pharmacokinetics, oral bioavailability and dose proportionality of ragaglitazar, a novel PPAR-dual activator in rats.
Chaluvadi, MR; Jagannath, K; Mamidi, NV; Mullangi, R; Srinivas, NR, 2004
)
0.32
"Allometric scaling has been used as an effective tool for the prediction of human pharmacokinetic parameters."( Preclinical pharmacokinetics and interspecies scaling of ragaglitazar, a novel biliary excreted PPAR dual activator.
Mullangi, R; Pavankuamr, VV; Srinivas, NR; Vinu, CA,
)
0.13

Bioavailability

ExcerptReferenceRelevance
" Compound 6 has also shown good oral bioavailability and impressive pharmacokinetic characteristics."( (-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
Bajji, AC; Chakrabarti, R; Juluri, S; Kalchar, S; Lohray, BB; Lohray, VB; Mamidi, NV; Misra, P; Padakanti, S; Poondra, RR; Rajagopalan, R; Vikramadithyan, RK, 2001
)
0.54
" In another study, a single intravenous bolus dose of ragaglitazar was given to rats (n=4) at 3 mg/kg dose following administration through the lateral tail vein in order to obtain the absolute oral bioavailability and clearance parameters."( Intravenous pharmacokinetics, oral bioavailability and dose proportionality of ragaglitazar, a novel PPAR-dual activator in rats.
Chaluvadi, MR; Jagannath, K; Mamidi, NV; Mullangi, R; Srinivas, NR, 2004
)
0.32

Dosage Studied

ExcerptRelevanceReference
" Plasma concentration versus time data were generated following oral and intravenous dosing and pharmacokinetic analysis was performed using non-compartmental analysis."( Intravenous pharmacokinetics, oral bioavailability and dose proportionality of ragaglitazar, a novel PPAR-dual activator in rats.
Chaluvadi, MR; Jagannath, K; Mamidi, NV; Mullangi, R; Srinivas, NR, 2004
)
0.32
" We examined early (precancerous) changes in the bladder urothelium of rats orally dosed with ragaglitazar, using a newly developed flow cytometric method."( Generalized cellular hypertrophy is induced by a dual-acting PPAR agonist in rat urinary bladder urothelium in vivo.
Andersen, HV; Brinck, PR; Guldberg, TS; Hegelund, AC; Iversen, L; Jensen, MB; Jørgensen, L; Nielsen, HS; Oleksiewicz, MB; Sjogren, I; Thinggaard, UK; Thorup, I, 2005
)
0.33
" In the present work, we demonstrate that a library of degradation products of ragaglitazar--a novel tricyclic-gamma-alkyloxyphenylpropionic acid with hypolipidemic and antidiabetic activity--observed in stability indicating samples of a solid dosage formulation by LC-MS can be produced in a one pot oxidation reaction."( High speed development work by preparation of an "in-hand" library of NMR-quantified degradation products.
Hansen, L; Malmstrøm, J; Olsen, H; Ryager, A, 2005
)
0.33
" Rats were dosed orally for 16 days with bladder carcinogenic (ragaglitazar) as well as non-bladder carcinogenic (fenofibrate and rosiglitazone) PPAR agonists and protein changes were assayed in the urinary bladder urothelium by Western blotting."( Biomarkers for early effects of carcinogenic dual-acting PPAR agonists in rat urinary bladder urothelium in vivo.
Egerod, FL; Iversen, L; Nielsen, HS; Oleksiewicz, MB; Storgaard, T; Thorup, I,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, peroxisome proliferator activated receptor gammaHomo sapiens (human)IC50 (µMol)0.09200.09200.09200.0920AID977608
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)IC50 (µMol)0.09200.00501.205110.0000AID156959
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Ki0.09000.00000.37905.6000AID238857
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)IC50 (µMol)0.98000.00050.82696.3100AID156285
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)Ki0.98000.00011.01894.5000AID238856
[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)
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)EC50 (µMol)3.20000.00200.47533.2000AID240312
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC50 (µMol)0.58000.00000.992210.0000AID1467416; AID156797; AID156934; AID223547; AID240313; AID717061
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)EC50 (µMol)3.13670.00061.607410.0000AID1467415; AID155986; AID156133; AID223541; AID240312; 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
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)
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 (50)

Assay IDTitleYearJournalArticle
AID156383Transcriptional activation of Peroxisome proliferator-activator receptor (PPAR) gamma expressed in HEK 293T cells at 1 uM2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID238856Binding 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.
AID25979Pharmacokinetic parameter in Male Wistar rats at 10 mg/kg oral administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1467415Agonist activity at GAL4 fused human PPARalpha LBD (174 to 475 residues) expressed in HEK293T cells after 18 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.
AID156133In vitro activation of human peroxisome proliferator activated receptor alpha2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID240312Effective 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.
AID156793Percent agonistic 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.
AID238857Binding affinity for human 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.
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.
AID223541In vitro transactivation using receptor transactivation assay against hPPAR alpha2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID1467416Agonist activity at GAL4 fused human PPARgamma LBD (174 to 475 residues) expressed in HEK293T cells after 18 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.
AID29704Pharmacokinetic parameter in Male Wistar rats at 10 mg/kg oral administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
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.
AID28334Pharmacokinetic parameter in Male Wistar rats at 10 mg/kg oral administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID28335Pharmacokinetic parameter in Male Wistar rats at 3 mg/kg intravenous administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID25980Pharmacokinetic parameter in Male Wistar rats at 3 mg/kg intravenous administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
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).
AID156382Transcriptional activation of Peroxisome proliferator-activator receptor (PPAR) alpha expressed in HEK 293T cells at 50 uM2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID27154Pharmacokinetic parameter in Male Wistar rats at 10 mg/kg oral administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID156299In vitro Fold activation relative to maximum activation obtained with WY-14643 (~ 20-fold corresponded to 100%) for human peroxisome proliferator activated receptor alpha2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID29106Pharmacokinetic parameter in Male Wistar rats at 3 mg/kg intravenous administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID625295Drug Induced Liver Injury Prediction System (DILIps) validation dataset; compound DILI positive/negative as observed in Pfizer data2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
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).
AID29105Pharmacokinetic parameter in Male Wistar rats at 10 mg/kg oral administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID223543Fold activation relative to maximum hPPAR alpha activation obtained with WY-146432002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID157111In vitro Fold activation relative to maximum activation obtained with rosiglitazone (~ 120-fold corresponded to 100%) for human peroxisome proliferator activated receptor gamma2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID29938Pharmacokinetic parameter in Male Wistar rats at 3 mg/kg intravenous administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID29829Pharmacokinetic parameter in Male Wistar rats at 10 mg/kg oral administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
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.
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.
AID223547In vitro transactivation using receptor transactivation assay against hPPAR gamma2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID223546Fold activation relative to maximum activation obtained with carbacyclin2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID223549Fold activation relative to maximum activation obtained with rosiglitazone2002Journal of medicinal chemistry, Feb-14, Volume: 45, Issue:4
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
AID155982Percent agonistic activity for human 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.
AID156934In vitro activation of human peroxisome proliferator activated receptor gamma (PPAR gamma)2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID27882Pharmacokinetic parameter in Male Wistar rats at 3 mg/kg intravenous administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID156778In vitro Fold activation relative to maximum activation obtained with carbacyclin (~ 250-fold corresponded to 100%) for human peroxisome proliferator activated receptor delta2003Bioorganic & medicinal chemistry letters, Jan-20, Volume: 13, Issue:2
Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template.
AID27155Pharmacokinetic parameter in Male Wistar rats at 3 mg/kg intravenous administration.2001Journal of medicinal chemistry, Aug-02, Volume: 44, Issue:16
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
AID240313Effective concentration against human 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.
AID1346733Human Peroxisome proliferator-activated receptor-alpha (1C. Peroxisome proliferator-activated receptors)2003Journal 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.
AID1346800Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors)2003British journal of pharmacology, Oct, Volume: 140, Issue:3
Ragaglitazar: a novel PPAR alpha PPAR gamma agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models.
AID1346800Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors)2003Journal 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.
AID1346800Human Peroxisome proliferator-activated receptor-gamma (1C. Peroxisome proliferator-activated receptors)2005British journal of pharmacology, Feb, Volume: 144, Issue:3
The dual PPARalpha/gamma agonist, ragaglitazar, improves insulin sensitivity and metabolic profile equally with pioglitazone in diabetic and dietary obese ZDF rats.
AID1811Experimentally measured binding affinity data derived from PDB2003Journal 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.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2003Journal 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (39)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's32 (82.05)29.6817
2010's7 (17.95)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (7.32%)5.53%
Reviews6 (14.63%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other32 (78.05%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]