货号	规格	价格	上海	北京	珠海	重庆	武汉
S88308-5mg促销	≥97%	￥618.00 ￥556.00 S88308-5mg ￥556.00 3-5天	0 货期：3-5天	-	-	-	-
S88308-25mg促销	≥97%	￥2360.00 ￥2130.00 S88308-25mg ￥2130.00 3-5天	0 货期：3-5天	-	-	-	-
S88308-100mg促销	≥97%	￥6020.00 ￥5420.00 S88308-100mg ￥5420.00 现货	5 5	-	-	-	-

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产品描述：

MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM

靶点：

AMPK:8 nM (EC50);AMPK

体外研究：

MK-3903 (compound 42) is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM. MK-3903 activates 10 of the 12 phosphorylated AMPK (pAMPK) complexes with EC50 values in the range of 8 to 40 nM and maximal activation >50%. MK-3903 partially activates pAMPK5 (36% max) and it does not activate pAMPK6. MK-3903 demonstrates low permeability (Papp=6×10-6 cm/s) in LLC-PK1 cells42 and is a substrate of human liver uptake transporters OATP1B1 and OATP1B3 (organic anion transporter proteins). Results show that MK-3903 binds moderately to the prostanoid DP2 (CRTH2) receptor (binding IC50=1.8 μM) but not in the presence of 10% human serum (binding IC50>86 μM)

体内研究：

The pharmacokinetics of MK-3903 (compound 42) in C57BL/6 mice, Sprague to Dawley rats, and beagle dogs are characterized by moderate systemic plasma clearance (5.0 to13 mL/min/kg), a volume of distribution at steady state of 0.6 to 1.1 L/kg, and a terminal halflife of ~2h. Acute oral administration of MK-3903 (3, 10, and 30 mg/kg) to high-fructose fed db/+ mice results in significant inhibition of hepatic fatty acid synthesis (FAS) for all three doses

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.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.198 ml	10.991 ml	21.983 ml
5 mM	0.44 ml	2.198 ml	4.397 ml
10 mM	0.22 ml	1.099 ml	2.198 ml
50 mM	0.044 ml	0.22 ml	0.44 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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