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产品描述： Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM. |
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靶点：
EC50: 72 nM (GPR40);GPR |
体内研究：
Fasiglifam (TAK-875) (10 mg/kg, p.o.) increases plasma insulin levels in ZDF rats. Fasiglifam (TAK-875) (30 mg/kg, p.o.) improves fasting hyperglycemia without affecting fasting normoglycemia. Fasiglifam (TAK-875) at 30 mg/kg, which is a 3- to 10-fold higher dose compared with the dose that improved glucose tolerance in diabetic rats, does not alter fasting glucose levels in SD rats with normal glucose homeostasis. Likewise, Fasiglifam (TAK-875) does not significantly alter insulin secretion in SD rats with normal fasting glucose levels |
参考文献：
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 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. 4. Urano Y, et al. Comparative hepatic transcriptome analyses revealed possible pathogenic mechanisms of fasiglifam (TAK-875)-induced acute liver injury in mice. Chem Biol Interact. 2018 Sep 20;296:185-197. |
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溶解性：
Soluble in DMSO |
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保存条件：
-20℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
1.906 ml |
9.53 ml |
19.061 ml |
| 5 mM |
0.381 ml |
1.906 ml |
3.812 ml |
| 10 mM |
0.191 ml |
0.953 ml |
1.906 ml |
| 50 mM |
0.038 ml |
0.191 ml |
0.381 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京