AMG 837 is a potent, orally bioavailable GPR40 agonist with EC50 of 14 nM.
|Source||Physiol Rep (2015). Figure 3. AMG-837|
|Cell Lines||rat small intestine|
|Results||Intergroup comparisons between LA, TAK-875, AMG 837, and DMSO stimulations showed that only the GLP-1 response induced by vascular AMG 837 was significantly different from the vehicle control|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Xihao Chang, et al. Collective synthesis of acetylenic pharmaceuticals via enantioselective Nickel/Lewis acid-catalyzed propargylic alkylation
 Sameer Mohammad. GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus: Benefits and Challenges
 Jonathan B Houze, et al. AMG 837: a potent, orally bioavailable GPR40 agonist
 Daniel C-H Lin, et al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents
 Ryo Yazaki, et al. Enantioselective synthesis of a GPR40 agonist AMG 837 via catalytic asymmetric conjugate addition of terminal alkyne to α,β-unsaturated thioamide
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