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10.1021/ml300063m

http://scihub22266oqcxt.onion/10.1021/ml300063m
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C4025728!4025728!24900499
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suck abstract from ncbi


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pmid24900499      ACS+Med+Chem+Lett 2012 ; 3 (6): 484-9
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  • The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes #MMPMID24900499
  • He S; Ye Z; Truong Q; Shah S; Du W; Guo L; Dobbelaar P; Lai Z; Liu J; Jian T; Qi H; Bakshi RK; Hong Q; Dellureficio J; Pasternak A; Feng Z; deJesus R; Yang L; Reibarkh M; Bradley S; Holmes MA; Ball RG; Ruck RT; Huffman M; Wong F; Samuel K; Reddy VB; Mitelman S; Tong S; Chicchi GG; Tsao KL; Trusca D; Wu M; Shao Q; Trujillo M; Eiermann GJ; Li C; Zhang BB; Howard A; Zhou YP; Nargund RP; Hagmann WK
  • ACS Med Chem Lett 2012[Jun]; 3 (6): 484-9 PMID24900499show ga
  • A structure?activity relationship study of the imidazolyl-?-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.
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