Omecamtiv mecarbil (Synonyms: CK-1827452; CK1827452)

Cell lines

Cardiac myocytes

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months.

Reaction Conditions

200 nM

Applications

Omecamtiv Mecarbil extended the duration of contraction without affecting the rates of contraction or relaxation. In addition, Omecamtiv Mecarbil also increased myocyte contraction in the presence of a β-adrenergic blocker, Carvedilol.

Animal models

Conscious and heart failure dogs

Dosage form

A bolus at 0.5 mg/kg, followed by infusion at 0.5 mg/kg per hr

Applications

In a conscious canine model, Omecamtiv Mecarbil improved left ventricular systolic function. In heart failure dogs, Omecamtiv Mecarbil significantly increased stroke volume and cardiac output.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Malik FI1, Hartman JJ, Elias KA, Morgan BP, Rodriguez H, Brejc K, Anderson RL, Sueoka SH, Lee KH, Finer JT, Sakowicz R, Baliga R, Cox DR, Garard M,Godinez G, Kawas R, Kraynack E, Lenzi D, Lu PP, Muci A, Niu C, Qian X, Pierce DW, Pokrovskii M, Suehiro I, Sylvester S, Tochimoto T, Valdez C, Wang W,Katori T, Kass DA, Shen YT, Vatner SF, Morgans DJ. Cardiac myosin activation: a potential therapeutic approach for systolic heart failure. Science. 2011 Mar 18;331(6023):1439-43.