MK-3903

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Chemical Structure| 1219737-12-8 同义名 : -
CAS号 : 1219737-12-8
货号 : A724442
分子式 : C27H19ClN2O3
纯度 : 99%+
分子量 : 454.904
MDL号 : MFCD22572341
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(230.82 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 MK-3903 is a potent AMPK activator with EC50 value of 9nM and max AMP activation of 320%. MK-3903 exhibited effect on recombinant human pAMPK complexes α1 β1 γ1, α1 β1 γ2, α1 β1 γ3, α1 β2 γ1, α1 β2 γ2, α1 β2 γ3, α2 β1 γ1, α2 β1 γ2, α2 β1 γ3, α2 β2 γ1, α2 β2 γ2 and α2 β2 γ3 units with EC50 value/max (%) of 8nM/217%, 21nM/242%, 19nM/61%, 40nM/50%, 118nM/36%, 2860nM/8%, 9nM/320%, 22nM/175%, 26nM/209%, 39nM/94%, 23nM/145% and 35nM/135%, respectively. Oral administration of MK-3903 at dose of 30mg/kg, BID, for 15days significantly increased the level of phosphorylated ACC, a downstream AMPK substrate as an indicator of intracellular AMPK activation, in liver and muscle of diet-induced obese mice. The hepatic fatty acid synthesis was inhibited by 29%, 37% and 49% in db/+mice dosed of 3, 10 and 30mg/kg MK-3903 post 8h. Oral dose of 10 and 30mg/kg MK-3903, BID, for 12 days resulted reduction of insulin resistance index of diet-induced obese mice up to 35% and 64% in an oral glucose tolerance test.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

10.99mL

2.20mL

1.10mL

21.98mL

4.40mL

2.20mL
参考文献

[1]Lan P, Romero FA, et al. Hit-to-Lead Optimization and Discovery of 5-((5-([1,1'-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase. J Med Chem. 2017 Nov 9;60(21):9040-9052.