Omecamtiv mecarbil

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Chemical Structure| 873697-71-3 同义名 : CK-1827452
CAS号 : 873697-71-3
货号 : A408772
分子式 : C20H24FN5O3
纯度 : 99%+
分子量 : 401.43
MDL号 : MFCD18633260
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
生物活性
描述 Omecamtiv mecarbil at 10 μM reduces the maximum rate of ATP hydrolysis (kcat) by 4.5-fold and lowers the actin concentration needed for half-maximal ATPase activity (KATPase) by 30-fold. The EC50 of Omecamtiv mecarbil-induced inhibition of actin-activated ATPase is determined to be 0.52 ± 0.10 μM. It does not alter overall actin affinity but causes a state of weak actin affinity in a subset of myosin heads with slow product release. In an in vitro motility assay, it reduces the actin sliding velocity by more than 100-fold[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.49mL

0.50mL

0.25mL

12.46mL

2.49mL

1.25mL

24.91mL

4.98mL

2.49mL
参考文献

[1]Morgan BP, et al. Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin. ACS Med Chem Lett. 2010 Aug 20;1(9):472-7.

[2]Mamidi R, et al. Molecular effects of the myosin activator omecamtiv mecarbil on contractile properties of skinned myocardium lacking cardiac myosin binding protein-C. J Mol Cell Cardiol. 2015 Aug;85:262-72.

[3]Swenson AM, et al. Omecamtiv Mecarbil Enhances the Duty Ratio of Human β-Cardiac Myosin Resulting in Increased Calcium Sensitivity and Slowed Force Development in Cardiac Muscle. J Biol Chem. 2017 Mar 3;292(9):3768-3778.