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Description: Fasiglifam (also known as TAK-875) is a novel, long-acting, selective and orally bioavailable and selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, it is 400-fold more potent than oleic acid. TAK-875 has a favorable pharmacokinetic profile which enables long-acting drug efficacy. TAK-875 exhibited potent agonistic activity and high binding affinity to the human GPR40 receptor. In addition, TAK-875 showed excellent agonist potency and selectivity for GPR40 receptor over other members of the FFA receptor family (e.g. EC50> 10 uM for others).
References: ACS Med Chem Lett. 2010 Jun 18; 1(6):290-4; J Pharmacol Exp Ther. 2011 Oct; 339(1):228-37.
Related CAS#: 1374598-80-7 (hydrate)
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