Dofetilide

Modify Date: 2024-01-02 20:51:09

Dofetilide Structure
Dofetilide structure
Common Name Dofetilide
CAS Number 115256-11-6 Molecular Weight 441.565
Density 1.3±0.1 g/cm3 Boiling Point 614.1±65.0 °C at 760 mmHg
Molecular Formula C19H27N3O5S2 Melting Point 147-1490C
MSDS Chinese USA Flash Point 325.2±34.3 °C
Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Danger

 Use of Dofetilide


Dofetilide(Tikosyn) is a class III antiarrhythmic agent.Target: Potassium ChannelIn patients with congestive heart failure and reduced left ventricular function, dofetilide was effective in converting atrial fibrillation, preventing its recurrence, and reducing the risk of hospitalization for worsening heart failure. Dofetilide had no effect on mortality [1]. dofetilide preferentially blocks open (or activated) channels and that the fast inactivation may competitively slow the binding kinetics. Dofetilide acts as a slow-onset/slow-offset open channel blocker of this current at nanomolar concentrations [2].

 Names

Name dofetilide
Synonym More Synonyms

 Dofetilide Biological Activity

Description Dofetilide(Tikosyn) is a class III antiarrhythmic agent.Target: Potassium ChannelIn patients with congestive heart failure and reduced left ventricular function, dofetilide was effective in converting atrial fibrillation, preventing its recurrence, and reducing the risk of hospitalization for worsening heart failure. Dofetilide had no effect on mortality [1]. dofetilide preferentially blocks open (or activated) channels and that the fast inactivation may competitively slow the binding kinetics. Dofetilide acts as a slow-onset/slow-offset open channel blocker of this current at nanomolar concentrations [2].
Related Catalog
References

[1]. Maisch, B., et al., [Pregnancy and cardiomyopathies]. Herz, 2003. 28(3): p. 196-208.

[2]. Snyders, D.J. and A. Chaudhary, High affinity open channel block by dofetilide of HERG expressed in a human cell line. Mol Pharmacol, 1996. 49(6): p. 949-55.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 614.1±65.0 °C at 760 mmHg
Melting Point 147-1490C
Molecular Formula C19H27N3O5S2
Molecular Weight 441.565
Flash Point 325.2±34.3 °C
Exact Mass 441.139221
PSA 121.57000
LogP 1.56
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.614
Storage condition Store at RT

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
PB0478000
CHEMICAL NAME :
Methanesulfonamide, N-(4-(2-(methyl(2-(4-((methylsulfonyl)amino)phenoxy)e thyl)amino)ethyl) phenyl)-
CAS REGISTRY NUMBER :
115256-11-6
LAST UPDATED :
199806
DATA ITEMS CITED :
3

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
22050 ug/kg
SEX/DURATION :
female 11 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 53,168,1996
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
11025 ug/kg
SEX/DURATION :
female 13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 53,168,1996
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
44100 ug/kg
SEX/DURATION :
female 14 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
REFERENCE :
TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 53,168,1996

 Safety Information

Symbol GHS07 GHS08
GHS07, GHS08
Signal Word Danger
Hazard Statements H302-H360
Precautionary Statements P201-P308 + P313
Hazard Codes Xi
Risk Phrases R36/37/38:Irritating to eyes, respiratory system and skin .
Safety Phrases 26-37/39
RIDADR NONH for all modes of transport

 Articles52

More Articles
Synchronous systolic subcellular Ca2+-elevations underlie ventricular arrhythmia in drug-induced long QT type 2.

Circ. Arrhythm. Electrophysiol. 8 , 703-12, (2015)

Repolarization delay is a common clinical problem, which can promote ventricular arrhythmias. In myocytes, abnormal sarcoplasmic reticulum Ca(2+)-release is proposed as the mechanism that causes early...

The Link between Inactivation and High-Affinity Block of hERG1 Channels.

Mol. Pharmacol. 87 , 1042-50, (2015)

Block of human ether-à-go-go-related gene 1 (hERG1) K(+) channels by many drugs delays cardiac repolarization, prolongs QT interval, and is associated with an increased risk of cardiac arrhythmia. Pre...

Relevance of calmodulin/CaMKII activation for arrhythmogenesis in the AV block dog.

Heart Rhythm 9(11) , 1875-83, (2012)

The calcium-dependent signaling molecules calcineurin and calcium/calmodulin-dependent protein kinase II (CaMKII) both have been linked to decompensated hypertrophy and arrhythmias. CaMKII is also bel...

 Synonyms

N-[4-[2-[Methyl[2-[4-[(methylsulfonyl)amino]phenoxy]ethyl]amino]ethyl]phenyl]methanesulfon Amide
Dofetilidum
Xelide
N-[4-[2-[2-[4-(methanesulfonamido)phenoxy]ethyl-methylamino]ethyl]phenyl]methanesulfonamide
MFCD00869707
Dofetilide
1-MSPMPE
b-((p-Methanesulfonamidophenethyl)methylamino)methanesulfono-p-phenetidide
N-(4-{2-[Methyl(2-{4-[(methylsulfonyl)amino]phenoxy}ethyl)amino]ethyl}phenyl)methanesulfonamide
Dofetilida
Methanesulfonamide, N-[4-[2-[methyl[2-[4-[(methylsulfonyl)amino]phenoxy]ethyl]amino]ethyl]phenyl]-
Tikosyn
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