TAK-875 (Fasiglifam) - GPR40 Agonist. CAS# 1374598-80-7 0083 targeting Smoothened (Smo) with an

targeting Smoothened (Smo) with an EC50 ~1 nM

BAY11-7082

2(5):611-24

AZ20 potently inhibits the growth of LoVo colorectal adenocarcinoma tumor cells in vitro and has high free exposure in mouse following moderate oral doses

K858 induces mitotic arrest and growth inhibition via the activation of the Mad2-mediated spindle checkpoint

TAK-875 (Fasiglifam) - GPR40 Agonist. CAS# 1374598-80-7 0083 targeting Smoothened (Smo) with anTAK 875 (Fasiglifam), CAS No. 1374598 80 7, is the potent, selective and orally bioavailable partial GPR40 agonist with an EC50 ~14 nM. It has binding affinity to the human GPR40 receptor with Ki of 38 nM and the rat GPR40 receptor with Ki of 140 nM. TAK 875 has no agonist potency to other members of the FFA receptor family with EC50 >10 M. The 2. 3 resolution co complex structure of hGPR40 TAK 875 reveals a unique binding mode of TAK 875 and suggests