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Aficamten (CK-274)

Cat. No. M19970
Aficamten (CK-274) Structure
Synonym:

CK-3773274; CK-274

Size Price Availability Quantity
5mg USD 270  USD270 In stock
10mg USD 420  USD420 In stock
25mg USD 800  USD800 In stock
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Quality Control & Documentation
Biological Activity

Aficamten (CK-274, CK 3773274) is a novel cardiac myosin inhibitor that reduces myocardial contractile force in vitro and in vivo with an IC50 of 1.4 μM.

Chemical Information
Molecular Weight 337.38
Formula C18H19N5O2
CAS Number 2364554-48-1
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Ashley N Sharpe, et al. Sci Rep. Effects of Aficamten on cardiac contractility in a feline translational model of hypertrophic cardiomyopathy

[2] Ashley N Sharpe, et al. J Vet Pharmacol Ther. Pharmacokinetics of a single dose of Aficamten (CK-274) on cardiac contractility in a A31P MYBPC3 hypertrophic cardiomyopathy cat model

[3] Chihyuan Chuang, et al. J Med Chem. Discovery of Aficamten (CK-274), a Next-Generation Cardiac Myosin Inhibitor for the Treatment of Hypertrophic Cardiomyopathy

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Keywords: Aficamten (CK-274), CK-3773274; CK-274 supplier, Myosin, inhibitors, activators


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