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Sematilide hydrochloride

Cat. No. M8906
Sematilide hydrochloride Structure
Synonym:

CK-1752 hydrochloride

Size Price Availability
10mg USD 250  USD250 1-2 Weeks
50mg USD 550  USD550 1-2 Weeks
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Quality Control & Documentation
Biological Activity

Sematilide (CK-1752) hydrochloride is a novel class III antiarrhythmic agent. Sematilide inhibits the rapidly activating delayed rectifier K+ current. The Ca2+-independent transient K+ and the inward rectifier K+ currents were not affected significantly by application of 100 microM sematilide. Moreover, voltage-dependent Na+ and Ca2+ currents were not affected significantly by 100 microM sematilide.

These findings indicate that sematilide selectively blocks the rapidly activating delayed rectifier K+ current in atrial myocytes and provide evidence supporting the usefulness of the drug as a class III antiarrhythmic agent. Application of 10, 30, 100 and 300 microM sematilide caused a concentration-dependent inhibition of the delayed rectifier K+ current (IC50 approx. 25 microM).

Chemical Information
Molecular Weight 349.87
Formula C14H24ClN3O3S
CAS Number 101526-62-9
Form Solid
Solubility (25°C) DMSO
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] Ishii Y, et al. Eur J Pharmacol. Effects of sematilide, a novel class III antiarrhythmic agent, on membrane currents in rabbit atrial myocytes.

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