MK-0941 free base

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MK-0941 free base

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

752240-01-0

MK-0941 free base 是具有口服活性的葡糖激酶 (glucokinase) 抑制剂，在葡萄糖浓度为 2.5 和 10 mM 的条件下，对重组人 glucokinase 的EC₅₀值分别为 240 和 65 nM。MK-0941 free base 具有较强的降血糖活性，是研究 2 型糖尿病的候选药物。

生物活性

MK-0941 free base is an orally activeglucokinaseactivator, withEC₅₀s of 240 and 65 nM for recombinant humanglucokinasein the presence of 2.5 and 10 mM glucose, respectively. MK-0941 free base exhibits strong glucose-lowering activity and is a potential therapeutic agent for treatment of type 2 diabetes^[1]^[2].

IC₅₀& Target

Glucokinase^[1]^[2].

体内研究
(In Vivo)

MK-0941 free base (3 or 10 mg/kg, sing oral dose) treatment reduced blood glucose significantly indb/dbdiabetic mouse^[1].

Animal Model:	Maledb/dbanddb/+ (lean) mice (9-10 weeks of age, weighing 43-45 g)^[1].
Dosage:	3 or 10 mg/kg.
Administration:	Oral gavage, single dose.
Result:	Resulted in significant reduction in blood glucose. These two doses lowered blood glucose similarly at 1 h after dosing, suggesting that saturation of effect was approached.

Clinical Trial

分子量

460.50

Formula

C₂₁H₂₄N₄O₆S

CAS 号

752240-01-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.