2830607-59-3
Chemical Structure
Ulacamten
Synonym(s): CK-4021586; CK-586
- CAS No.: 2830607-59-3
- Formula:C21H25F2N3O3
- Molecular Weight:405.44
InChIKey: HLMGUFOCTBBSLK-KOMQPUFPSA-N
SMILES: O=C(N([C@@H]1CC[C@H](CC1)C)CC2=O)C3(CN(C3)C=O)N2CC4=CC(F)=C(C=C4)F
Biological Activity: Ulacamten (CK-4021586; CK-586) is an orally active cardiac myosin inhibitor and an inhibitor of the double-headed cardiac heavy meromyosin (HMM)ATPase (excluding single-headed myosin subfragment-1), with an EC50 of 2.9 μM. Ulacamten regulates cardiac myosin, reduces excessive myocardial contractility, and alleviates left ventricular outflow tract obstruction. Ulacamten increases the left ventricular short-axis systolic internal diameter, inhibits dobutamine-induced exacerbation of obstruction, and exerts only a mild reducing effect on left ventricular systolic function. Ulacamten also inhibits the fractional shortening of the short axis without altering calcium transients. Ulacamten shows good safety and tolerability in purpose-bred cats with naturally occurring obstructive hypertrophic cardiomyopathy[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Ulacamten | 99.22% | Ulacamten (CK-4021586; CK-586) is an orally active cardiac myosin inhibitor and an inhibitor of the double-headed cardiac heavy meromyosin (HMM)ATPase (excluding single-headed myosin subfragment-1), with an EC50 of 2.9 μM. Ulacamten regulates cardiac myosin, reduces excessive myocardial contractility, and alleviates left ventricular outflow tract obstruction. Ulacamten increases the left ventricular short-axis systolic internal diameter, inhibits dobutamine-induced exacerbation of obstruction, and exerts only a mild reducing effect on left ventricular systolic function. Ulacamten also inhibits the fractional shortening of the short axis without altering calcium transients. Ulacamten shows good safety and tolerability in purpose-bred cats with naturally occurring obstructive hypertrophic cardiomyopathy. | ||||||||||||||||||||
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References
- [1]. Rivas VN, et al. Cardiac myosin inhibitor, CK-586, minimally reduces systolic function and ameliorates obstruction in feline hypertrophic cardiomyopathy. Sci Rep. 2024;14(1):12038. Published 2024 May 27. [Content Brief]
- [2]. Sarkar S S, et al. Preclinical characterization of CK-4021586, a new class of cardiac myosin inhibitors for the treatment of hypertrophic cardiomyopathy[J]. Biophysical Journal, 2023, 122(3): 122a.
