| Identification | Back Directory | [Name]
TAK875 | [CAS]
1374598-80-7 | [Synonyms]
CS-1926
TAK-875(0.5H2O)
TAK875 hemihydrate
TAK-875 hymihydrate
(3S)-6-[[2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-3-benzofuranacetic acid hydrate (2:1)
[(3S)-6-({2',6'-dimethyl-4'-[3-(methylsulfonyl)propoxy]biphe-nyl-3-yl}meth-oxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid hemi-hydrate
TAK875 (3S)-6-[[2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-3-benzofuranacetic acid | [Molecular Formula]
C29H32O7S.1/2H2O | [MDL Number]
MFCD18251445 | [MOL File]
1374598-80-7.mol | [Molecular Weight]
1067.27 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 100 mg/mL (187.40 mM);Ethanol: Insoluble | [Water Solubility ]
Water: Insoluble | [InChIKey]
OJXYMYYDAVXPIK-IWKNALKQSA-N | [CAS DataBase Reference]
1374598-80-7 |
| Hazard Information | Back Directory | [Characteristics]
More potent at activating hGPR40 than oleic acid | [Uses]
Fasiglifam (TAK-875) hemihydrate is a potent, selective and orally active GPR40 agonist with EC50 of 72 nM. Fasiglifam enhances glucose-dependent insulin secretion and improves hyperglycemia in type 2 diabetic rats. Fasiglifam can induce liver injury[1][2][3][4]. | [Biological Activity]
TAK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid. | [target]
| Target | Value | GPR40
(CHO cells expressing human GPR40) | < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> 14 nM(EC50)
| [storage]
Store at -20°C | [References]
[1] Tsujihata Y,et al. TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats.J Pharmacol Exp DOI:10.1124/jpet.111.183772
[2] Yoshiyuki Tsujihata, et al. TAK-875, an Orally Available GPR40/FFA1 Agonist Enhances Glucose-Dependent Insulin Secretion and Improves Both Postprandial and Fasting Hyperglycemia in Type 2 Diabetic Rats. JPET July 13, 2011
[3] Nagatake T, et al. 17,18-EpETE-GPR40 axis ameliorates contact hypersensitivity by inhibiting neutrophil mobility in mice and cynomolgus macaques. J Allergy Clin Immunol. 2017 Dec 26. pii: S0091-6749(17)32949-4. DOI:10.1016/j.jaci.2017.09.053 |
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