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101526-62-9

101526-62-9 structure
101526-62-9 structure
  • Name: Sematilide hydrochloride
  • Chemical Name: N-[2-(diethylamino)ethyl]-4-(methanesulfonamido)benzamide,hydrochloride
  • CAS Number: 101526-62-9
  • Molecular Formula: C14H24ClN3O3S
  • Molecular Weight: 349.87700
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Potassium Channel
  • Create Date: 2018-08-23 11:59:27
  • Modify Date: 2024-01-12 14:52:07
  • Sematilide hydrochloride (CK-1752 hydrochloride) 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].
Name N-[2-(diethylamino)ethyl]-4-(methanesulfonamido)benzamide,hydrochloride
Synonyms Sematilide HCl
SEMATILIDE HYDROCHLORIDE
CK 1752A
Benzamide,N-(2-(diethylamino)ethyl)-4-((methylsulfonyl)amino)-,monohydrochloride
N-[2-(diethylamino)ethyl]-4-[(methylsulfonyl)amino]benzamide hydrochloride
Sematilide hydrochloride (USAN)
N-(2-(Diethylamino)ethyl)-4-((methylsulfonyl)amino)benzamide monohydrochloride
Sematilide monohydrochloride
[14C]-Sematilide hydrochloride
Description Sematilide hydrochloride (CK-1752 hydrochloride) 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
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.
Boiling Point 511.9ºC at 760 mmHg
Molecular Formula C14H24ClN3O3S
Molecular Weight 349.87700
Flash Point 263.4ºC
Exact Mass 349.12300
PSA 86.89000
LogP 3.47640
Vapour Pressure 7.59E-11mmHg at 25°C
Storage condition -20℃

CHEMICAL IDENTIFICATION

RTECS NUMBER :
CV4203840
CHEMICAL NAME :
Benzamide, N-(2-(diethylamino)ethyl)-4-((methylsulfonyl)amino)-, monohydrochloride
CAS REGISTRY NUMBER :
101526-62-9
LAST UPDATED :
199603
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C14-H23-N3-O3-S.Cl-H
MOLECULAR WEIGHT :
349.92

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3200 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
92 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1800 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
96 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
500 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
143 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
90 gm/kg/90D-I
TOXIC EFFECTS :
Related to Chronic Data - death
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
27 gm/kg/90D-I
TOXIC EFFECTS :
Behavioral - ataxia Gastrointestinal - nausea or vomiting Related to Chronic Data - death
REFERENCE :
CDREEA Cardiovascular Drug Reviews. (Raven Press, 1185 Avenue of the Americas, New York, NY 10036) V.6- 1988- Volume(issue)/page/year: 10,182,1992
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