916220-04-7Relevant academic research and scientific papers
Discovery of the imidazole-derived GPR40 agonist AM-3189
Ma, Zhihua,Lin, Daniel C.-H.,Sharma, Rajiv,Liu, Jinqian,Zhu, Liusheng,Li, An-Rong,Kohn, Todd,Wang, Yingcai,Liu, Jiwen,Bartberger, Michael D.,Medina, Julio C.,Zhuang, Run,Li, Frank,Zhang, Jane,Luo, Jian,Wong, Simon,Tonn, George R.,Houze, Jonathan B.
, p. 15 - 20 (2015/12/18)
As a follow-up to the GPR40 agonist AMG 837, which was evaluated in clinical trials for the treatment of type II diabetes, further optimization led to the discovery of AM-3189 (13k). AM-3189 is representative of a new class of compounds with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837.
Optimization of GPR40 agonists for type 2 diabetes
Liu, Jiwen,Wang, Yingcai,Ma, Zhihua,Schmitt, Mike,Zhu, Liusheng,Brown, Sean P.,Dransfield, Paul J.,Sun, Ying,Sharma, Rajiv,Guo, Qi,Zhuang, Run,Zhang, Jane,Luo, Jian,Tonn, George R.,Wong, Simon,Swaminath, Gayathri,Medina, Julio C.,Lin, Daniel C.-H.,Houze, Jonathan B.
, p. 517 - 521 (2014/06/09)
GPR40 (FFA1 and FFAR1) has gained significant interest as a target for the treatment of type 2 diabetes. TAK-875 (1), a GPR40 agonist, lowered hemoglobin A1c (HbA1c) and lowered both postprandial and fasting blood glucose levels in type 2 diabetic patient
