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Omecamtiv mecarbil

Cat. No. M2004
Omecamtiv mecarbil Structure
Synonym:

CK-1827452

Size Price Availability Quantity
10mg USD 260 In stock
50mg USD 800 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Omecamtiv mecarbil, previously codenamed CK-1827452, is an agent that directly activates myosin, for use in the treatment of heart failure. Omecamtiv mecarbil specifically targets and activates myocardial ATPase and improves energy utilization. This enhances effective myosin cross-bridge formation and duration, while the velocity of contraction remains the same. Omecamtiv mecarbil also increases the rate of phosphate release from myosin, thereby accelerating the rate-determining step of the cross-bridge cycle, which is the transition of the actin-myosin complex from the weakly bound to the strongly bound state. Omecamtiv mecarbil could safely improve cardiac function within tolerated doses. Omecamtiv mecarbil is currently in Phase II clinical trials.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 401.43
Formula C20H24FN5O3
CAS Number 873697-71-3
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

The effects of the cardiac myosin activator, omecamtiv mecarbil, on cardiac function in systolic heart failure: a double-blind, placebo-controlled, crossover, dose-ranging phase 2 trial.
Cleland JG, et al. Lancet. 2011 Aug 20;378(9792):676-83. PMID: 21856481.

Dose-dependent augmentation of cardiac systolic function with the selective cardiac myosin activator, omecamtiv mecarbil: a first-in-man study.
Teerlink JR, et al. Lancet. 2011 Aug 20;378(9792):667-75. PMID: 21856480.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Omecamtiv mecarbil, CK-1827452 supplier, ATPase, inhibitors

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