Omarigliptin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Omarigliptin(MK-3102) 是一种有效、选择性、长效的 DPP-4 抑制剂，IC50 为 1.6 nM；对所有测试的蛋白酶具有高度选择性 (IC50 > 67 μM)。

Omarigliptin(MK-3102) is a potent, selective and long-acting DPP-4 inhibitor with IC50 of 1.6 nM; highly selective over all proteases tested (IC50 > 67 μM). IC50 value: 1.6 nM Target: DPP-4 inhibitor in vitro: Omarigliptin has weak ion channel activity (IC50 > 30 μM at IKr, Cav1.2, and Nav1.5). An expansive selectivity counterscreen (168 radioligand binding or enzymatic assays) was carried out at MDS Pharma. An IC50 > 10 μM was obtained in all assays. in vivo: When orally administered 1 h prior to dextrose challenge in an oral glucose tolerance test (OGTT), it significantly reduced blood glucose excursion in a dose-dependent manner from 0.01 mg/kg (7% reduction in glucose AUC) to 0.3 mg/kg (51% reduction).

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MK-3102

Metabolic Enzyme/Protease

Other Targets

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1226781-44-7

398.43

C??H??F?N?O?S

>98% (HPLC)

DMSO : 50 mg/mL (125.49 mM; Need ultrasonic)

N[C@@H]1[C@@H](C2=CC(F)=CC=C2F)OC[C@H](N3CC4=NN(S(=O)(C)=O)C=C4C3)C1

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(-20℃)

With Ice Pack

≥ 2 years