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多非利特

多非利特用途

Dofetilide(Tikosyn)是III型抗心律失常药,能阻断钾离子通道。

多非利特名称

[ CAS 号 ]:
115256-11-6

[ 中文名 ]:
多非利特

[ 英文名 ]:
Dofetilide

[中文别名 ]:

[英文别名 ]:

Dofetilidum
Xelide
MFCD00869707
Dofetilide
1-MSPMPE
Dofetilida
Tikosyn

多非利特生物活性

[ 描述 ]:

Dofetilide(Tikosyn)是III型抗心律失常药,能阻断钾离子通道。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 心血管疾病

[参考文献]

[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.

[相关活性小分子]

多非利特物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
614.1±65.0 °C at 760 mmHg

[ 熔点 ]:
147-1490C

[ 分子式 ]:
C₁₉H₂₇N₃O₅S₂

[ 分子量 ]:
441.565

[ 闪点 ]:
325.2±34.3 °C

[ 精确质量 ]:
441.139221

[ PSA ]:
121.57000

[ LogP ]:
1.56

[ 外观性状 ]:
灰白色或淡黄色结晶粉末

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.614

[ 储存条件 ]:
Store at RT

多非利特MSDS

多非利特毒性和生态

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

多非利特安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H360

[ 警示性声明 ]:
P201-P308 + P313

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
26-37/39

[ 危险品运输编码 ]:
NONH for all modes of transport

多非利特合成路线

多非利特上下游产品

多非利特上游产品

多非利特下游产品

多非利特制备

将N-甲基-4-硝基苯乙胺与2-[4-硝基苯氧基]乙溴溶于乙腈,加入碳酸钾和碘化钠,搅拌回流反应.浓缩至干,剩余的油性固体经后处理得到化合物.将得到的化合物溶于乙醇,用Raney镍催化反应.过滤,滤液浓缩至干.经处理得到的化合物和甲磺酸酐溶于二氯甲烷,在室温下搅拌.生成物经进一步处理得到多非利特.

多非利特文献

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...

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