1104604-48-9Relevant academic research and scientific papers
The discovery of MK-4256, a potent SSTR3 antagonist as a potential treatment of type 2 diabetes
He, Shuwen,Ye, Zhixiong,Truong, Quang,Shah, Shrenik,Du, Wu,Guo, Liangqin,Dobbelaar, Peter H.,Lai, Zhong,Liu, Jian,Jian, Tianying,Qi, Hongbo,Bakshi, Raman K.,Hong, Qingmei,Dellureficio, James,Pasternak, Alexander,Feng, Zhe,Dejesus, Reynalda,Yang, Lihu,Reibarkh, Mikhail,Bradley, Scott A.,Holmes, Mark A.,Ball, Richard G.,Ruck, Rebecca T.,Huffman, Mark A.,Wong, Frederick,Samuel, Koppara,Reddy, Vijay B.,Mitelman, Stan,Tong, Sharon X.,Chicchi, Gary G.,Tsao, Kwei-Lan,Trusca, Dorina,Wu, Margaret,Shao, Qing,Trujillo, Maria E.,Eiermann, George J.,Li, Cai,Zhang, Bei B.,Howard, Andrew D.,Zhou, Yun-Ping,Nargund, Ravi P.,Hagmann, William K.
, p. 484 - 489 (2012/10/08)
A structure-activity relationship study of the imidazolyl-β- tetrahydrocarboline series identified MK-4256 as a potent, selective SSTR3 antagonist, which demonstrated superior efficacy in a mouse oGTT model. MK-4256 reduced glucose excursion in a dose-dependent fashion with maximal efficacy achieved at doses as low as 0.03 mg/kg po. As compared with glipizide, MK-4256 showed a minimal hypoglycemia risk in mice.
