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2',3'-二脱氧胞苷

2',3'-二脱氧胞苷用途

Zalcitabine是有效的核苷类似物逆转录酶抑制剂,用于治疗HIV感染。

2',3'-二脱氧胞苷名称

[ CAS 号 ]:
7481-89-2

[ 中文名 ]:
2,3-二脱氧胞啶

[ 英文名 ]:
Zalcitabine

[中文别名 ]:

[英文别名 ]:

ddCyd
[3H]-Zalcitabine
2',3'-DIDEOXYCYTIDINE
DDC
DDC (VAN)
Zalcitabine
HIVID
MFCD00012188
Cytidine,2',3'-dideoxy
Dideoxycytidine

2',3'-二脱氧胞苷生物活性

[ 描述 ]:

Zalcitabine是有效的核苷类似物逆转录酶抑制剂,用于治疗HIV感染。

[ 相关类别 ]:

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

[ 靶点 ]

Target: HIV

[体外研究]

Zalcitabine是一种双脱氧核苷抗逆转录病毒药,在未感染和HIV感染的细胞内磷酸化为活性代谢产物2',3'-双脱氧胞苷5'-三磷酸(ddCTP)。在治疗浓度下,ddCTP通过抑制酶逆转录酶和终止原病毒DNA链的延伸来抑制HIV复制[1]。 Zalcitabine对CHO/hOAT1细胞中[3H] -PAH的细胞摄取具有抑制作用,IC50值为1.23 mM。此外,随着CHO/hOAT1细胞中hOATI活性的增强,对于zalcitabine的细胞摄取增加了三倍[2]。

[参考文献]

[1]. Adkins JC, et al. Zalcitabine. An update of its pharmacodynamic and pharmacokinetic properties and clinical efficacy in the management of HIV infection.Drugs. 1997 Jun;53(6):1054-80

[2]. Jin MJ, et al. Interaction of zalcitabine with human organic anion transporter 1. Pharmazie. 2006 May;61(5):491-2.

[相关活性小分子]

2',3'-二脱氧胞苷物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
415.0±55.0 °C at 760 mmHg

[ 熔点 ]:
217-218 °C(lit.)

[ 分子式 ]:
C₉H₁₃N₃O₃

[ 分子量 ]:
211.218

[ 闪点 ]:
204.8±31.5 °C

[ 精确质量 ]:
211.095688

[ PSA ]:
90.37000

[ LogP ]:
-1.30

[ 外观性状 ]:
白色至灰白色结晶粉末

[ 蒸汽压 ]:
0.0±2.2 mmHg at 25°C

[ 折射率 ]:
1.686

[ 储存条件 ]:
2-8°C

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

[ 水溶解性 ]:
5-10 g/100 mL at 19 ºC

2',3'-二脱氧胞苷MSDS

详细MSDS(安全技术说明书)

2',3'-二脱氧胞苷毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HA3870000

CHEMICAL NAME :: Cytidine, 2',3'-dideoxy-

CAS REGISTRY NUMBER :: 7481-89-2

BEILSTEIN REFERENCE NO. :: 0654956

LAST UPDATED :: 199712

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C9-H13-N3-O3

MOLECULAR WEIGHT :: 211.25

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 188 gm/kg/94D-I

TOXIC EFFECTS :: Blood - changes in bone marrow (not otherwise specified) Blood - changes in erythrocyte (RBC) count Blood - changes in leukocyte (WBC) count

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 94 gm/kg/94D-I

TOXIC EFFECTS :: Blood - other changes Blood - changes in other cell count (unspecified) Blood - changes in erythrocyte (RBC) count

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 14500 mg/kg/29D-I

TOXIC EFFECTS :: Blood - other changes Blood - changes in other cell count (unspecified) Blood - changes in erythrocyte (RBC) count

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 91 mg/kg/13W-I

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Endocrine - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 10 gm/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 20 gm/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death

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

2',3'-二脱氧胞苷安全信息

[ 符号 ]:

GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H351

[ 警示性声明 ]:
P280

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R40

[ 安全声明 (欧洲) ]:
S22-S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
HA3870000

[ 海关编码 ]:
2934999090

2',3'-二脱氧胞苷合成路线

详细合成路线

2',3'-二脱氧胞苷上下游产品

2',3'-二脱氧胞苷上游产品

2',3'-二脱氧胞苷下游产品

2',3'-二脱氧胞苷制备

N-乙酰基胞嘧啶核苷(4g，14mmo1)在200ml乙腈中回流，在30min内滴加乙酰溴(10ml，0.137mo1)，加毕再回流3h。蒸出溶剂，剩余物溶于100ml氯仿后，用100ml水洗。蒸去氯仿，剩余物用10ml乙醇重结晶，得2g无色片状结晶的化合物(I)，收率33%，熔点179-180℃(分解)。
化合物(I)(1g，2.3mmo1)、lg碳酸钙、0.2g钯-硫酸钡和50ml 50%甲醇，在25℃和常压下与氢气摇晃1h(吸收60ml氢)。过滤除去结晶，滤液浓缩至干。剩余物溶于10ml 20%氨-甲醇溶液，于5℃下放置过夜。柱层析后再用乙醇重结晶，得34mg无色结晶的扎西他滨，收率7%。

2',3'-二脱氧胞苷海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

2',3'-二脱氧胞苷文献

Absence of a universal mechanism of mitochondrial toxicity by nucleoside analogs.

Antimicrob. Agents Chemother. 51 , 2531-9, (2007)

Nucleoside analogs are associated with various mitochondrial toxicities, and it is becoming increasingly difficult to accommodate these differences solely in the context of DNA polymerase gamma inhibi...

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...

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