Compounds > sipoglitazar
Page last updated: 2024-12-11

sipoglitazar

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

Description

sipoglitazar: an antidiabetic agent [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9825652
CHEMBL ID3526439
SCHEMBL ID5380746
MeSH IDM0573718

Synonyms (30)

Synonym
3-[3-ethoxy-1-[[4-[(2-phenyl-1,3-thiazol-4-yl)methoxy]phenyl]methyl]pyrazol-4-yl]propanoic acid
sipoglitazar [inn]
unii-40o898cjzb
3-(3-ethoxy-1-((4-((2-phenyl-1,3-thiazol-4-yl)methoxy)phenyl)methyl)pyrazol-4-yl)propanoic acid
sipoglitazar
3-(3-ethoxy-1-(4-((2-phenyl-1,3-thiazol-4-yl)methoxy)benzyl)-1h-pyrazol-4-yl)propanoic acid
40o898cjzb ,
342026-92-0
FT-0674598
tak-654
3-(3-ethoxy-1-{4-[(2-phenyl-1,3-thiazol-4-yl)methoxy]benzyl}-1h-pyrazol-4-yl)propanoic acid
SRFCAWATPLCLMG-UHFFFAOYSA-N
3-[3-ethoxy-1-[4-(2-phenyl-4-thiazolylmethoxy)benzyl]-1h-pyrazol-4-yl]propionic acid
SCHEMBL5380746
AC-33692
3-[3-ethoxy-1-[4-[(2-phenyl-1,3-thiazol-4-yl)methoxy]benzyl]-1h-pyrazol-4-yl]propionic acid
CHEMBL3526439
AKOS030528585
3-[3-ethoxy-1-({4-[(2-phenyl-1,3-thiazol-4-yl)methoxy]phenyl}methyl)-1h-pyrazol-4-yl]propanoic acid
J-019495
3-ethoxy-1-[[4-[(2-phenyl-4-thiazolyl)methoxy]phenyl]methyl]-1h-pyrazole-4-propanoic acid
EX-A2440
3-(3-ethoxy-1-(4-((2-phenylthiazol-4-yl)methoxy)benzyl)-1h-pyrazol-4-yl)propanoic acid
A11783
BCP33099
tak-654; tak 654; tak654
Q27258344
DTXSID50870331
HY-103034
CS-0023370

Research Excerpts

Overview

Sipoglitazar is a novel anti-diabetic agent with triple agonistic activities on the human peroxisome proliferator-activated receptors, hPPAR-γ, -α, and -δ.

ExcerptReferenceRelevance
"Sipoglitazar is a peroxisome proliferator-activated receptor α, δ, and γ agonist. "( Evaluation of the impact of UGT polymorphism on the pharmacokinetics and pharmacodynamics of the novel PPAR agonist sipoglitazar.
Danhof, M; DeJongh, J; Karim, A; Ploeger, BA; Scott, G; Stringer, F; Urquhart, R, 2013)		2.04
"Sipoglitazar is a novel anti-diabetic agent with triple agonistic activities on the human peroxisome proliferator-activated receptors, hPPAR-γ, -α, and -δ. "( Metabolic fate of sipoglitazar, a novel oral PPAR agonist with activities for PPAR-γ, -α and -δ, in rats and monkeys and comparison with humans in vitro.
Asahi, S; Kamiguchi, H; Kawaguchi, N; Kiyota, Y; Kondo, T; Maeshiba, Y; Nishihara, M; Sudo, M; Tagawa, Y; Takahashi, J, 2012)		2.16

Pharmacokinetics

ExcerptReferenceRelevance
" Plasma samples were collected for up to 48 h post-dose to characterize the pharmacokinetic profile following a single oral dose of the drug."( The effect of genetic polymorphisms in UGT2B15 on the pharmacokinetic profile of sipoglitazar, a novel anti-diabetic agent.
Kinley, J; Nishihara, M; Scott, G; Stringer, F; Urquhart, R; Valbuena, M, 2013)		0.62
" The impact of genotype on exposure was assessed using a pharmacokinetic modeling approach; the influence of genotype on efficacy was evaluated using 12-week HbA1c change from baseline."( Evaluation of the impact of UGT polymorphism on the pharmacokinetics and pharmacodynamics of the novel PPAR agonist sipoglitazar.
Danhof, M; DeJongh, J; Karim, A; Ploeger, BA; Scott, G; Stringer, F; Urquhart, R, 2013)		0.6
" The aim of the current analysis was to apply a PK-PD model-based approach to evaluate the influence of UGT2B15 driven pharmacokinetic differences on the clinical response."( A model-based approach to analyze the influence of UGT2B15 polymorphism driven pharmacokinetic differences on the pharmacodynamic response of the PPAR agonist sipoglitazar.
Danhof, M; DeJongh, J; Scott, G; Stringer, F, 2014)		0.6

Bioavailability

ExcerptReferenceRelevance
" The bioavailability for sipoglitazar was 95."( Metabolic fate of sipoglitazar, a novel oral PPAR agonist with activities for PPAR-γ, -α and -δ, in rats and monkeys and comparison with humans in vitro.
Asahi, S; Kamiguchi, H; Kawaguchi, N; Kiyota, Y; Kondo, T; Maeshiba, Y; Nishihara, M; Sudo, M; Tagawa, Y; Takahashi, J, 2012)		1.02
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID1209547Drug metabolism in human hepatic microsomes assessed as formation of 3-[3-ethoxy-1-(4-hydroxybenzyl)-1H-pyrazol-4-yl]propanoic acid] at 10 uM after 6 hrs by LC-MS and LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209554Drug metabolism in human hepatic microsomes assessed as formation of 3-(3-hydroxy-1-{4-[(2-phenyl-1,3-thiazol-4-yl)methoxy]benzyl}-1H-pyrazol-4-yl)propanoic acid at 10 uM after 6 hrs by LC-MS and LC-MS/MS analysis in presence of NADPH2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209574Drug metabolism in human hepatic microsomes assessed as elimination of compound at 10 uM after 30 mins by LC-MS and LC-MS/MS analysis in presence of gemfibrozil, NADPH and UDPGA2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209580Drug metabolism in human hepatic microsomes assessed as elimination of compound at 10 uM after 30 mins by LC-MS and LC-MS/MS analysis in presence of gemfibrozil and UDPGA2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209579Drug metabolism in human hepatic microsomes assessed as beta-1-O-acyl glucuronide conjugate of sipoglitazar formation at 10 uM after 30 mins by LC-MS and LC-MS/MS analysis in presence of gemfibrozil and UDPGA2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209573Drug metabolism in human hepatic microsomes assessed as formation of 3-[3-ethoxy-1-(4-hydroxybenzyl)-1H-pyrazol-4-yl]propanoic acid] at 10 uM after 30 mins by LC-MS and LC-MS/MS analysis in presence of gemfibrozil, NADPH and UDPGA2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209548Drug metabolism in cryopreserved primary human hepatocytes assessed as formation of 3-(3-hydroxy-1-{4-[(2-phenyl-1,3-thiazol-4-yl)methoxy]benzyl}-1H-pyrazol-4-yl)propanoic acid at 10 uM after 6 hrs by LC-MS and LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209549Drug metabolism in cryopreserved primary human hepatocytes assessed as formation of 3-[3-ethoxy-1-(4-hydroxybenzyl)-1H-pyrazol-4-yl]propanoic acid] at 10 uM after 6 hrs by LC-MS and LC-MS/MS analysis2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209558Drug metabolism in human hepatic microsomes assessed as formation of alpha-2-O-acyl glucuronide conjugate of sipoglitazar at 100 uM after 4 hrs by HPLC analysis in presence of UDPGA2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209551Drug metabolism in human hepatic microsomes assessed as formation of 3-(3-hydroxy-1-{4-[(2-phenyl-1,3-thiazol-4-yl)methoxy]benzyl}-1H-pyrazol-4-yl)propanoic acid at 10 uM after 6 hrs by LC-MS and LC-MS/MS analysis in presence of NADPH and UDPGA2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209557Drug metabolism in human hepatic microsomes assessed as formation of beta-1-O-acyl glucuronide conjugate of sipoglitazar at 100 uM after 4 hrs by HPLC analysis in presence of UDPGA2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209552Drug metabolism in human hepatic microsomes assessed as formation of 3-[3-ethoxy-1-(4-hydroxybenzyl)-1H-pyrazol-4-yl]propanoic acid] at 10 uM after 6 hrs by LC-MS and LC-MS/MS analysis in presence of NADPH and UDPGA2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
AID1209572Drug metabolism in human hepatic microsomes assessed as formation of 3-(3-hydroxy-1-{4-[(2-phenyl-1,3-thiazol-4-yl)methoxy]benzyl}-1H-pyrazol-4-yl)propanoic acid at 10 uM after 30 mins by LC-MS and LC-MS/MS analysis in presence of gemfibrozil, NADPH and U2012Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2
An unusual metabolic pathway of sipoglitazar, a novel antidiabetic agent: cytochrome P450-catalyzed oxidation of sipoglitazar acyl glucuronide.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's6 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 65.80

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index65.80 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index107.18 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (65.80)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (50.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other3 (50.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
oxazepam
Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5.		2.08101,4-benzodiazepinone;
organochlorine compound		anxiolytic drug;
environmental contaminant;
xenobiotic
thiazoles
[no description available]		5.64631,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
uridine diphosphate glucuronic acid
Uridine Diphosphate Glucuronic Acid: A nucleoside diphosphate sugar which serves as a source of glucuronic acid for polysaccharide biosynthesis. It may also be epimerized to UDP iduronic acid, which donates iduronic acid to polysaccharides. In animals, UDP glucuronic acid is used for formation of many glucosiduronides with various aglycones.. UDP-alpha-D-glucuronic acid : A UDP-sugar having alpha-D-glucuronic acid as the sugar component.		2.0710UDP-D-glucuronic acidEscherichia coli metabolite;
human metabolite;
mouse metabolite
rosiglitazone
[no description available]		3.4811aminopyridine;
thiazolidinediones		EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
insulin-sensitizing drug
ConditionIndicatedRelationship StrengthStudiesTrials
Diabetes Mellitus, Adult-Onset
[description not available]		04.4422
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		04.4422