AMG-3969,1361224-53-4

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AMG-3969

CAS No. : 1361224-53-4

MCE 国际站：AMG-3969

产品活性：AMG-3969是有效的葡萄糖激酶-葡糖激酶调节蛋白(GK-GKRP)相互作用的干扰物，IC₅₀值为4 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Glucokinase

In Vitro: AMG-3969 exhibits potent cellular activity with an EC₅₀ of 0.202 μM and IC₅₀ of 4 nM, . It potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation in vitro (isolated hepatocytes).

In Vivo: AMG-3969 has good in vivo pharmacokinetic (PK) properties in rats (75%) and significantly lowers blood glucose levels in a dose-dependent manner db/db mice. AMG-3969 (100 mg/kg) demonstrates significant reductions in blood glucose with robust efficacy (56% reduction) observed at the 8 h time point. AMG-3969 demonstrates dose-dependent efficacy in three models of diabetes: diet induced obese (DIO), ob/ob and db/db mice; however,AMG-3969 is ineffective in lowering blood glucose in normoglycaemic C57BL/6 (B6) mice. AMG-3969 is highly effective in promoting carbohydrate substrate. AMG-3969 exhibits extended changes to carbohydrate oxidation as observed by increased respiratory exchange ratio into the next night and day after a single dose.

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