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Omecamtiv mecarbil

Catalog No. T2006 CAS 873697-71-3

Synonyms: CK-1827452

Omecamtiv mecarbil (CK-1827452) has been used in trials studying the treatment and basic science of Heart Failure, Echocardiogram, Pharmacokinetics, Chronic Heart Failure, and History of Chronic Heart Failure, among others.

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Omecamtiv mecarbil, CAS 873697-71-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 77.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 207.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 549.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 99.62%

Purity: 98.75%

Purity: 98%

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Storage & Solubility Information

Description	Omecamtiv mecarbil (CK-1827452) has been used in trials studying the treatment and basic science of Heart Failure, Echocardiogram, Pharmacokinetics, Chronic Heart Failure, and History of Chronic Heart Failure, among others.
In vitro	Omecamtiv mecarbil induces a decrease in various hemodynamic parameters, including heart rate, mean left atrial pressure, and left ventricular end-diastolic pressure. The effects of Omecamtiv mecarbil on these hemodynamic parameters within dogs with left ventricular hypertrophy, while awake, show similar impacts without significant statistical differences. In conscious dogs with myocardial infarction (MI-sHF), Omecamtiv mecarbil significantly increases wall thickening (25%), stroke volume (44%), cardiac output (22%), and left ventricular (LV) contraction ejection time (26%).
In vivo	In isolated cardiomyocytes, Omecamtiv mecarbil (can) enhance(s) the contractility of myocytes, overcoming the inhibition of myosin by BDM without increasing calcium transients or inhibiting the PDE pathway. Ex-vivo, Omecamtiv mecarbil selectively activates cardiac myosin by increasing the rate of myosin ATPase, thereby enhancing myocardial contractility.
Kinase Assay	Axl Kinase activity assay: Test compounds are diluted to desired concentrations in kinase reaction buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT, and 0.01% v/v Tween-20) and are briefly incubated with Axl kinase. The Axl kinase used is recombinant human Axl kinase (catalytic domain, amino acids 473-894) with a histidine tag. The reaction is initiated by the addition of ATP and fluorescein-labeled poly-GT substrate (poly Glu:Tyr, 4:1 polymer). Concentration of the various components in the assay (10 μL reaction volume) are: 1% DMSO, 93 ng/mL Axl kinase, 20 μM ATP, and 200 nM fluorescein poly-GT substrate. Following addition of ATP and fluorescein poly-GT substrate, incubation is for 60 min at room temperature, the enzyme reaction is stopped by addition of 10 μL terbium-labeled anti-phosphotyrosine PY20 antibody in EDTA-containing buffer. Final concentration of EDTA and antibody after addition to the reaction is 10 mM and 2 nM, respectively. The terbium conjugated antibody generates a time-resolved FRET signal with the fluorescein molecule (bound to the poly-GT substrate) when the substrate is phosphorylated. After one hour incubation at room temperature, fluorescence is measured with excitation of 320 nm and dual emission of 495 and 520 nm on an EnVision microplate reader. Signal is expressed in -636996terms of a TR-FRET ratio (fluorescence intensity at 520 nm to 495 nm).

Synonyms	CK-1827452
Molecular Weight	401.43
Formula	C20H24FN5O3
CAS No.	873697-71-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 6 mg/mL (14.94 mM)

DMSO: 74 mg/mL (184.3 mM)

References and Literature

1. Anderson RL, et al. Mol Bio Cell, 2005, 16 (Abstract #1728). 2. Shen YT, et al. Circ Heart Fail. 2010, 3(4), 522-577.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Mitochondria-Targeted Compound Library Cytoskeletal Signaling Pathway Compound Library ReFRAME Related Library Target-Focused Phenotypic Screening Library Bioactive Compound Library Clinical Compound Library Anti-Cardiovascular Disease Compound Library

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Keywords

Omecamtiv mecarbil 873697-71-3 Cytoskeletal Signaling Membrane transporter/Ion channel ATPase Myosin CK-1827452 CK1827452 Inhibitor inhibit CK 1827452 inhibitor

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