Omecamtiv mecarbil (CK-1827452)

Catalog No.S2623

Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.

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Omecamtiv mecarbil (CK-1827452) Chemical Structure

Omecamtiv mecarbil (CK-1827452) Chemical Structure
Molecular Weight: 401.43

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Omecamtiv mecarbil (CK-1827452) is available in the following compound libraries:

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Product Description

Biological Activity

Description Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure. Phase 2.
Targets Myosin ATPase [1]
In vitro In vitro, Omecamtiv mecarbil selectively activates cardiac myosin by increasing the myosin ATPase rate. [1] In isolated cardiac myocytes, Omecamtiv mecarbil results in increase of myocyte contractility and overcomes of the myosin inhibitor BDM without increasing the calcium transient or inhibiting the PDE pathway. [1]
In vivo Omecamtiv mecarbil significantly increases fractional shortening starting at 0.4 mM plasma concentrations in SD rats, sham animals and in rats with heart failure. [1] In conscious dogs with myocardial infarction (MI-sHF), Omecamtiv mecarbil leads to a significant increase in wall thickening (25%), stroke volume (44%), cardiac output (22%) and left ventricular (LV) systolic ejection time (26%). In addition, Omecamtiv mecarbil also results in the decreases of some hemodynamic parameters including heart rate, mean left atrial pressure, and LV end-diastolic pressure. In conscious dogs with left ventricular hypertrophy (LVH-sHF), Omecamtiv mecarbil leads to similar and not statistically different effects on hemodynamic parameters. [2]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Biochemical assays Cardiac S1 myosin and thin filament proteins (actin, troponin complex, and tropomyosin) are prepared from bovine heart or rabbit skeletal muscle. Smooth muscle myosin is prepared from chicken gizzard. ATPase assays are performed in a kinetic fashion using NADH coupled enzyme system at pCa2+ = 6.75. Rates are normalized to a DMSO control.

Animal Study: [1]

Animal Models Sprague Dawley rats.
Formulation Omecamtiv mecarbil is dissolved in DMSO and then diluted in water.
Dosages ≤1.2 mg/kg/hour
Administration Administered via i.v.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[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.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02695420 Recruiting Heart Failure With Reduced Ejection Fraction Amgen April 2016 Phase 2
NCT01786512 Completed Modified Release Oral Formulation|Left Ventricular Systolic Dysfunction|Chronic Heart Failure|History of Chronic Heart Failure|Left Ventricular Eje  ...more Modified Release Oral Formulation|Left Ventricular Systolic Dysfunction|Chronic Heart Failure|History of Chronic Heart Failure|Left Ventricular Ejection Fraction|Pharmacokinetics|Echocardiogram Amgen|Cytokinetics February 2013 Phase 2
NCT01300013 Completed Heart Failure Amgen|Cytokinetics April 2011 Phase 2
NCT01077167 Withdrawn Heart Failure Amgen July 2010 Phase 2
NCT00941681 Completed Heart Failure Cytokinetics April 2009 Phase 2

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Chemical Information

Download Omecamtiv mecarbil (CK-1827452) SDF
Molecular Weight (MW) 401.43
Formula

C20H24FN5O3

CAS No. 873697-71-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 80 mg/mL (199.28 mM)
Ethanol 6 mg/mL (14.94 mM)
Water <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck 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.
Chemical Name methyl 4-(2-fluoro-3-(3-(6-methylpyridin-3-yl)ureido)benzyl)piperazine-1-carboxylate

Tech Support

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