Sematilide

Names

[ Name ]:
Sematilide

[Synonym ]:
C14H23N3O3S
UNII-0NHB13IN3R
Sematilide

Biological Activity

[Description]:

Sematilide (CK-1752) is a selective IKr channel blocker. Sematilide causes a concentration-dependent inhibition of the delayed rectifier K+ current (IC50=25 μM). Sematilide is a class III antiarrhythmic agent[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

IC50: 25 μM (K+ current)[1]

[In Vitro]

Application of 10, 30, 100 and 300 μM Sematilide causes a concentration-dependent inhibition of the delayed rectifier K+ current (IC50=25 μM)[1].

[In Vivo]

Sematilide (0.3-1.0 mg/kg, intravenously i.v.) is effective in a canine model of arrhythmia[2]. Animal Model: Mongrel dogs of either sex (10-18 kg body weight)[2] Dosage: 0.3, 1, 3, and 10 mg/kg Administration: I.v. infusions Result: Demonstrated antiarrhythmic effects at 0.3 and 3.0 mg/kg.

[References]

[1]. Ishii Y, et al. Effects of Sematilide, a novel class III antiarrhythmic agent, on membrane currents in rabbit atrial myocytes. Eur J Pharmacol. 1997 Jul 23;331(2-3):295-302.

[2]. Stanley S. Greenberg, et al. Pharmacology of Sematilide, a non-quaternary class III antiarrhythmic agent.

Chemical & Physical Properties

[ Density]:
1.205 g/cm3

[ Melting Point ]:
141-142 °C

[ Molecular Formula ]:
C₁₄H₂₃N₃O₃S

[ Molecular Weight ]:
313.41600

[ Exact Mass ]:
313.14600

[ PSA ]:
86.89000

[ LogP ]:
2.67440

[ Index of Refraction ]:
1.558

Safety Information

[ HS Code ]:
2935009090

Synthetic Route

Click to get detail synthetic route

Customs

[ HS Code ]: 2935009090

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%