CK-1827452 (Omecamtiv mecarbil)

Catalog No. A11206

CK-1827452 (Omecamtiv mecarbil)是选择性的心脏特异性肌球蛋白激活剂。

Product Citations

Oleg Lookin, .et al. Omecamtiv mecarbil attenuates length-tension relationship in healthy rat myocardium and preserves it in monocrotaline-induced pulmonary heart failure, Clin Exp Pharmacol Physiol, 2021, Aug 29 PMID: 34459025
Gabor A. Fulop, .et al. Omecamtiv mecarbil evokes diastolic dysfunction and leads to periodic electromechanical alternans, Basic Res Cardiol, 2021, 116(1): 24 PMID: 33844095
Wanjian Tang, .et al. Dilated cardiomyopathy mutation in the converter domain of human cardiac myosin alters motor activity and response to omecamtiv mecarbil, J Biol Chem, 2019, October 2 PMID: 31578282
Thinh T. Kieu, .et al. Omecamtiv Mecarbil Slows Myosin Kinetics in Skinned Rat Myocardium at Physiological Temperature, Biophysical Journal, 2019, 2019 PMID: 31103235
Alexandre J. S. Ribeiro, .et al. Multi-Imaging Method to Assay the Contractile Mechanical Output of Micropatterned Human iPSC-Derived Cardiac Myocytes, Circ Res, 2017, May 12; 120(10): 1572-1583 PMID: 28400398
Anja M. Swenson, .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 PMID: 28082673
Nánási P Jr, .et al. Omecamtiv mecarbil activates ryanodine receptors from canine cardiac but not skeletal muscle, Eur J Pharmacol, 2017, Aug 15;809:73-79 PMID: 28506910
Horv??th B, .et al. Frequency-dependent effects of omecamtiv mecarbil on cell shortening of isolated canine ventricular cardiomyocytes, Naunyn Schmiedebergs Arch Pharmacol, 2017, Dec;390(12):1239-1246 PMID: 28940010
Szentandrassy N, .et al. Dose-dependent electrophysiological effects of the myosin activator omecamtiv mecarbil in canine ventricular cardiomyocytes, J Physiol Pharmacol, 2016, Aug;67(4):483-489 PMID: 27779469
L Nagy, .et al. The novel cardiac myosin activator omecamtiv mecarbil increases the calcium sensitivity of force production in isolated cardiomyocytes and skeletal muscle fibres of the rat, Br J Pharmacol, 2015, Sep; 172(18): 4506-4518 PMID: 26140433
Larissa Butler, .et al. Enhanced characterization of contractility in cardiomyocytes during early drug safety assessment, Toxicol Sci, 2015, Jun;145(2):396-406 PMID: 25820236

Technical details

Catalog Num	A11206
M. Wt	401.43
Formula	C20H24FN5O3
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	873697-71-3
Synonyms	CK1827452, Omecamtiv Mecarbil
SMILES	CC1=NC=C(C=C1)NC(=O)NC2=CC=CC(=C2F)CN3CCN(CC3)C(=O)OC

Biological Activity

CK-1827452 (Omecamtiv mecarbil)是选择性的心脏特异性肌球蛋白激活剂。

Targets

Myosin ATPase

Solubility *

In vitro (25°C)	DMSO	73 mg/mL (181.84 mM)
	Water	Insoluble
	Ethanol	5 mg/mL (12.45 mM)
In vivo	1% DMSO+30% polyethylene glycol+1% Tween 80	28 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	24.91 mL	124.55 mL	249.11 mL
0.5 mM	4.98 mL	24.91 mL	49.82 mL
1 mM	2.49 mL	12.46 mL	24.91 mL
5 mM	0.5 mL	2.49 mL	4.98 mL

*The above data is based on the productmolecular weight 401.43. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.