MK-3903

MK-3903CAS号: 1219737-12-8分子式: C27H19ClN2O3分子量: 454.90描述纯度储存/保存方法可溶性/溶解性In vitro(体外研究)

产品描述
描述
MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM.
纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO : ≥ 100 mg/mL (219.83 mM)
生物活性
In vitro(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).

分子结构图

MK-3903