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司他夫定

司他夫定用途

Stavudine是核苷类似物,能抑制HIV逆转录酶。

司他夫定名称

[ CAS 号 ]:
3056-17-5

[ 中文名 ]:
司他夫定

[ 英文名 ]:
Stavudine

[中文别名 ]:

[英文别名 ]:

Sanilvudine
Virostav
Stavudine
Stauvidine
3'-Deoxy-2'-thymidinene
Zerit
2',3'-dideoxy-2',3'-didehydrothymidine
Thymidine, 2',3'-didehydro-3'-deoxy-
2',3'-didehydro-3'-deoxythimidine
D 4T

司他夫定生物活性

[ 描述 ]:

Stavudine是核苷类似物,能抑制HIV逆转录酶。

[ 相关类别 ]:

信号通路 >> 自噬 >> 自噬

信号通路 >> 抗感染 >> HIV

信号通路 >> 抗感染 >> 逆转录酶

研究领域 >> 感染

[参考文献]

[1]. Lea AP, et al. Stavudine: a review of its pharmacodynamic and pharmacokinetic properties and clinical potential in HIV infection. Drugs. 1996 May;51(5):846-64.

[2]. Igoudjil A, et al. High doses of stavudine induce fat wasting and mild liver damage without impairing mitochondrial respiration in mice. Antivir Ther. 2007;12(3):389-400.

[相关活性小分子]

司他夫定物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
440.6±55.0 °C at 760 mmHg

[ 熔点 ]:
159-160°C

[ 分子式 ]:
C₁₀H₁₂N₂O₄

[ 分子量 ]:
224.213

[ 闪点 ]:
220.3±31.5 °C

[ 精确质量 ]:
224.079712

[ PSA ]:
84.32000

[ LogP ]:
-1.25

[ 外观性状 ]:
白色粉末

[ 蒸汽压 ]:
0.0±2.4 mmHg at 25°C

[ 折射率 ]:
1.646

[ 储存条件 ]:
−20°C

[ 稳定性 ]:
Stable. Combustible. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
5-10 g/100 mL at 21 ºC

司他夫定MSDS

司他夫定毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XP2075000

CHEMICAL NAME :: Thymidine, 2',3'-didehydro-3'-deoxy-

CAS REGISTRY NUMBER :: 3056-17-5

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C10-H12-N2-O4

MOLECULAR WEIGHT :: 224.24

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 600 mg/kg/3D (Continuous)

REFERENCE :: EMMUEG Environmental and Molecular Mutagenesis. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.10- 1987- Volume(issue)/page/year: 18,168,1991

司他夫定安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

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

[ WGK德国 ]:
2

[ RTECS号 ]:
XP2075000

[ 海关编码 ]:
2938901000

司他夫定合成路线

司他夫定上下游产品

司他夫定上游产品

司他夫定下游产品

司他夫定制备

胸苷溶于无水吡啶，冰盐冷却下滴加甲磺酰氯，搅拌、过滤，真空干燥，得磺酰化粗品。粗品用90％乙醇重结晶，得精品。将上述磺酰化产物溶于氢氧化钠水溶液，回流。用盐酸中和，蒸去溶剂，残液加氯仿，滤除不溶物，蒸去氯仿，用乙酸、乙醇结晶，得。色固体的环氧物。用乙醇重结晶2次可得白色絮状固体。将该环氧物溶于二甲亚砜，加入叔丁醇钾，在室温下搅拌。用50％乙酸的乙醇溶液中和至pH＝7。减压浓缩，得到的物质用热丙酮洗涤。洗液过滤后浓缩，再加乙醇，活性炭脱色，过滤。蒸出乙醇，加少量苯旋转蒸发至溶液出现浑浊，静置。析出的固体用乙醇-苯(1:5)重结晶，得白色粉状的司他夫定。

司他夫定海关

[ 海关编码 ]: 2938901000

[ 中文概述 ]:
HS: 2938901000. 齐多夫定、拉米夫定、司他夫定、地达诺新及它们的盐. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最低关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 来源

[ Summary ]:
HS: 2938901000. 4-amino-1-((2r,5s)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl)pyrimidin-2(1h)-one. VAT:17.0%. tax rebate rate:13.0%. supervision conditions:None. MFN tarrif:6.5%. general tariff:20.0%

司他夫定文献

Both 2',3'-dideoxythymidine and its 2',3'-unsaturated derivative (2',3'-dideoxythymidinene) are potent and selective inhibitors of human immunodeficiency virus replication in vitro.

Biochem. Biophys. Res. Commun. 142 , 128, (1987)

2',3'-Dideoxythymidine (ddThd) and its 2',3'-unsaturated derivative 2',3'-dideoxythymidinene (ddeThd) are potent and selective inhibitors of human immunodeficiency virus (HIV) in vitro. When evaluated...

The separation and detection of PET tracers via capillary electrophoresis for chemical identity and purity analysis.

J. Pharm. Biomed. Anal. 94 , 12-8, (2014)

CE coupled with UV detection was assessed as a possible platform for the chemical identity and purity analysis of positron emission tomography (PET) tracers using [(18)F]FAC and [(18)F]FLT as examples...

Viral protein R of HIV type-1 induces retrotransposition and upregulates glutamate synthesis by the signal transducer and activator of transcription 1 signaling pathway.

Microbiol. Immunol. 59 , 398-409, (2015)

Viral protein R (Vpr) of HIV-1 plays an important role in viral replication in macrophages. Various lines of evidence suggest that expression of Vpr in macrophages causes immunopathogenesis; however, ...

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