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PPARgamma agonist

A PPAR modulator which activates the peroxisome proliferator-activated receptor-gamma.

ChEBI ID: 71554

Members (5)

MemberDefinitionClass
6,7,4'-trihydroxyisoflavoneA hydroxyisoflavone that is daidzein bearing an additional hydroxy substituent at position 6.4',6,7-trihydroxyisoflavone
monascinAn organic heterotricyclic compound that is 3a,4,8,9a-tetrahydro-2H-furo[3,2-g][2]benzopyran-2,9(3H)-dione that is substituted at positions 3, 6, and 9a by hexanoyl, (1E)-prop-1-en-1-yl and methyl groups, respectively (the 3S,3aR,9aR diastereoisomer). One of the azaphilonoid pigments in extracts of Monascus pilosus-fermented rice (red-mould rice), it is a potent inhibitor of carcinogenesis measured against chemical- or UV-initiated, phorbol-promoted mouse skin tumours.monascin
pioglitazoneA member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.pioglitazone
protectin d1A dihydroxydocosahexaenoic acid that is (4Z,7Z,11E,13E,15Z,19Z)-docosahexaenoic acid in which the two hydroxy substituents are located at positions 10 and 17 (the 10R,17S-stereoisomer). Protectin D1 is one of the specialised proresolving mediators. When produced in neural tissues, it is called neuroprotectin D1protectin D1
saroglitazarA monocarboxylic acid that is (2S)-2-ethoxy-3-(p-ethoxyphenyl)propanoic acid in which one of the methyl hydrogens of the p-ethoxy substituent has been replaced by the nitrogen of 2-methyl-5-[4-(methylthio)phenyl]-1H-pyrrole. An agonist at the subtypes alpha and gamma of the peroxisome proliferator-activated receptor (PPAR) with predominant PPARalpha activity, it is used in the treatment of type 2 diabetes.saroglitazar

Research

Studies (4,467)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19901 (0.02)18.7374
1990's135 (3.02)18.2507
2000's1,606 (35.95)29.6817
2010's2,190 (49.03)24.3611
2020's535 (11.98)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials837 (18.11%)5.53%
Reviews574 (12.42%)6.00%
Case Studies110 (2.38%)4.05%
Observational23 (0.50%)0.25%
Other3,078 (66.59%)84.16%

Protein Targets (40)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency15.848911
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency2.511911
EWS/FLI fusion proteinHomo sapiens (human)Potency0.155222
TDP1 proteinHomo sapiens (human)Potency26.101122
tyrosine-protein kinase YesHomo sapiens (human)Potency1.729111

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Amine oxidase [flavin-containing] AHomo sapiens (human)IC5035.069011
Amine oxidase [flavin-containing] A Rattus norvegicus (Norway rat)Ki0.270811
Amine oxidase [flavin-containing] BHomo sapiens (human)IC500.298022
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki0.323433
Amine oxidase [flavin-containing] BRattus norvegicus (Norway rat)Ki0.856733
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
Bile salt export pumpHomo sapiens (human)IC500.337066
Bile salt export pumpRattus norvegicus (Norway rat)IC502.000011
Carbonic anhydrase 2Homo sapiens (human)IC500.114011
Carnitine O-palmitoyltransferase 1, liver isoformHomo sapiens (human)IC5010.000011
Carnitine O-palmitoyltransferase 2, mitochondrialHomo sapiens (human)IC50100.000011
Carnitine O-palmitoyltransferase 2, mitochondrialRattus norvegicus (Norway rat)IC50100.000011
CDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)IC508.650011
CDGSH iron-sulfur domain-containing protein 1Rattus norvegicus (Norway rat)IC501.000011
CDGSH iron-sulfur domain-containing protein 1Homo sapiens (human)Ki0.370011
CDGSH iron-sulfur domain-containing protein 2Homo sapiens (human)IC504.800011
Enoyl-[acyl-carrier-protein] reductase [NADH] Francisella tularensis subsp. tularensis SCHU S4IC5079.000011
Multidrug resistance-associated protein 4Homo sapiens (human)IC5049.500011
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)IC5010.000011
Peroxisome proliferator-activated receptor alphaMus musculus (house mouse)IC501.150011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)IC505.408188
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)IC500.700011
Peroxisome proliferator-activated receptor gammaRattus norvegicus (Norway rat)IC500.700011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Ki0.576188
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)IC5070.000012
Polyunsaturated fatty acid lipoxygenase ALOX12Homo sapiens (human)IC508.700011
Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)IC5049.000011
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)IC5080.000023
Steryl-sulfataseHomo sapiens (human)IC500.800011
TyrosinaseMus musculus (house mouse)IC50500.000011
Tyrosine-protein phosphatase non-receptor type 1Homo sapiens (human)IC50220.000011
Xanthine dehydrogenase/oxidaseHomo sapiens (human)IC501,000.000022

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Free fatty acid receptor 1Homo sapiens (human)EC50812.831011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)EC500.550012
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)EC500.550012
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)EC500.550012
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)EC500.550012
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)EC500.550012
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)EC506.686733
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC500.80273636
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)EC500.620022
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Kd0.871011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Activity3.140022