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.
| Molecular Weight | 401.43 |
| Formula | C20H24FN5O3 |
| CAS Number | 873697-71-3 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related Myosin Products |
|---|
| Myosin Light Chain Kinase Substrate (smooth muscle)
Myosin Light Chain Kinase Substrate (smooth muscle) is a smooth muscle myosin light chain kinase (MLCK) synthetic peptide substrate. |
| Kemptamide
Kemptamide, a 13 amino acid fragment with a sequence corresponding to residues 11-23 of gizzard light chain. |
| MYK-224
MYK-224 is a cardiac myosin complex modulator that can be used in studies related to cardiovascular disease. |
| Myosin V-IN-1
Myosin V-IN-1 is a potent and selective Myosin V inhibitor, with a Ki of 6 μM. |
| 16-38-Thymosin β4 (cattle) TFA
16-38-Thymosin β4 (cattle) TFA is a non-Ca2+-dependent MLCK activator with high affinity. |
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