CAS 115256-11-6|Dofetilide

Introduction：Basic information about CAS 115256-11-6|Dofetilide, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Dofetilide BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Articles52
7. Synonyms

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	ChineseUSA	Flash Point	325.2±34.3 °C
Symbol	GHS07, GHS08	Signal Word	Danger

Names

Name	dofetilide
Synonym	More Synonyms

Dofetilide BiologicalActivity

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	Signaling Pathways >>Membrane Transporter/Ion Channel >>Potassium ChannelResearch Areas >>Cardiovascular Disease
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.

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

Signaling Pathways >>Membrane Transporter/Ion Channel >>Potassium ChannelResearch Areas >>Cardiovascular Disease

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
InChIKey	IXTMWRCNAAVVAI-UHFFFAOYSA-N
SMILES	CN(CCOc1ccc(NS(C)(=O)=O)cc1)CCc1ccc(NS(C)(=O)=O)cc1
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
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

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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