Fasiglifam (TAK-875) Hemihydrate manufacturers
|
| | Fasiglifam (TAK-875) Hemihydrate Basic information |
| Product Name: | Fasiglifam (TAK-875) Hemihydrate | | Synonyms: | [(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;TAK-875(0.5H2O);(3S)-6-[[2',6'-Dimethyl-4'-[3-(methylsulfonyl)propoxy][1,1'-biphenyl]-3-yl]methoxy]-2,3-dihydro-3-benzofuranacetic acid hydrate (2:1);TAK875 hemihydrate;CS-1926;TAK-875 hymihydrate;TAK-875（b） | | CAS: | 1374598-80-7 | | MF: | C58H66O15S2 | | MW: | 1067.26564 | | EINECS: | | | Product Categories: | API;Inhibitors | | Mol File: | 1374598-80-7.mol |  |
| | Fasiglifam (TAK-875) Hemihydrate Chemical Properties |
| 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 |
| | Fasiglifam (TAK-875) Hemihydrate Usage And Synthesis |
| 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)
| | 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 |
| | Fasiglifam (TAK-875) Hemihydrate Preparation Products And Raw materials |
|