Keywords

• AMG-3969
• AMG3969
• AMG 3969

Quick Details

• ProName: AMG-3969
• CasNo: 1361224-53-4
• Molecular Formula: C21H20F6N4O3S
• Application: For laboratory use only- not intended ...
• ProductionCapacity: 1 Kilogram/Quarter
• Purity: ≥98%
• Storage: room temperature
• Transportation: by air
• LimitNum: 5 Gram

Superiority

Details

AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC₅₀ of 4 nM. IC50 & Target: IC50: 4 nM (GK-GKRP).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.