1. Cytoskeleton
  2. Myosin
  3. Omecamtiv mecarbil

Omecamtiv mecarbil (Synonyms: CK-1827452)

Cat. No.: HY-14233 Purity: 99.28%
Handling Instructions

Omecamtiv mecarbil is a cardiac myosin activator.

For research use only. We do not sell to patients.

Omecamtiv mecarbil Chemical Structure

Omecamtiv mecarbil Chemical Structure

CAS No. : 873697-71-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 154 In-stock
Estimated Time of Arrival: December 31
5 mg USD 140 In-stock
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10 mg USD 270 In-stock
Estimated Time of Arrival: December 31
50 mg USD 823 In-stock
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100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
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Description

Omecamtiv mecarbil is a cardiac myosin activator.

In Vitro

Omecamtiv mecarbil (10 μM) reduces the maximal ATPase (kcat) 4.5-fold and dramatically reduces the actin concentration at which ATPase is half-maximal (KATPase) 30-fold. The Omecamtiv mecarbil-induced inhibition of the actin-activated ATPase is evaluated in a concentration-dependent manner to determine the EC50 (0.52 ± 0.10 μM). Omecamtiv mecarbil does not change the overall actin affinity. Omecamtiv mecarbil traps a population of myosin heads in a weak actin affinity state with slow product release. Omecamtiv mecarbil can reduce the actin sliding velocity more than 100-fold in the in vitro motility assay[3].

In Vivo

Omecamtiv mecarbil (100-1000 ng/mL) demonstrates concentration-dependent increases in FS in Sprague−Dawley rats model. Omecamtiv mecarbil demonstrates good PK parameters in both rats (Sprague−Dawley) and dogs (Beagle) with clearances of 22 and 7.2 mL/min/kg, volumes of 3.5 and 3.6 L/kg, and bioavailabilities (F%) of 100 and 80%, respectively[1]. Omecamtiv mecarbil does not affect the phosphorylation status of myofilament proteins in both WT and KO hearts as shown by the absence of significant differences between pre and post Omecamtiv mecarbil samples within WT and KO groups, or affect the force generation at maximal Ca2+ activation (pCa 4.5) in any of the groups. Omecamtiv mecarbil increases the responsiveness of the cardiac myofilaments to Ca2+ at submaximal Ca2+-activations[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (124.55 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4911 mL 12.4555 mL 24.9109 mL
5 mM 0.4982 mL 2.4911 mL 4.9822 mL
10 mM 0.2491 mL 1.2455 mL 2.4911 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.23 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

401.43

Formula

C₂₀H₂₄FN₅O₃

CAS No.

873697-71-3

SMILES

O=C(N1CCN(CC1)CC2=C(C(NC(NC3=CC=C(N=C3)C)=O)=CC=C2)F)OC

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Omecamtiv mecarbil
Cat. No.:
HY-14233
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Omecamtiv mecarbil

Cat. No.: HY-14233