索立夫定
索立夫定用途
Sorivudine (BV-araU) 是一种口服活性的,合成的嘧啶核苷抗代谢 (pyrimidine nucleoside antimetabolite) 药物。Sorivudine 的抗病毒活性来自某些 DNA 病毒中存在的特定胸苷激酶 (thymidine kinase) 选择性转化为核苷酸,从而反过来会干扰病毒 DNA 合成 (DNA synthesis)。
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索立夫定名称
[ CAS 号 ]:
77181-69-2
[ 中文名 ]:
索立夫定
[ 英文名 ]:
Sorivudine
[英文别名 ]:
- Bravavir
- Bravavir (tn)
- Sorivudin
- YN-72
- Brovavir
- BV-araU
索立夫定生物活性
[ 描述 ]:
Sorivudine (BV-araU) 是一种口服活性的,合成的嘧啶核苷抗代谢 (pyrimidine nucleoside antimetabolite) 药物。Sorivudine 的抗病毒活性来自某些 DNA 病毒中存在的特定胸苷激酶 (thymidine kinase) 选择性转化为核苷酸,从而反过来会干扰病毒 DNA 合成 (DNA synthesis)。
[ 相关类别 ]:
[体外研究]
索里夫定(BV-araU)对ID50s(50%抑制剂量)分别为0.39μM和0.67μM的HSV-1和HSV-2(野生型VR-3和UW-268)的抑制作用[1]。索里夫定对水痘-带状疱疹病毒、单纯疱疹1型病毒和爱泼斯坦-巴尔病毒等几种病毒具有抗病毒活性[1]。索里夫定(BV-araU)是一种嘧啶核苷类似物,对水痘带状疱疹病毒(VZV)有体外抑制作用,其浓度为00001-0.004 mg/ml,比阿昔洛韦3抑制VZV复制所需浓度低1000倍以上浓度范围为0.03-0.1 mg/ml[2]。
[体内研究]
索里夫定(BV-araU)经口给药治疗HSV-l脑炎。当剂量超过12.5mg/kg时,治疗小鼠的存活时间延长。当剂量超过50mg/kg时,死亡率显著降低(we1l),一个更相关的模型是非洲绿猴(cerophiccus aethiops)的猴水痘病毒感染。在这个系统中,索里夫定的治疗剂量低至20毫克/千克/天肌肉注射或100毫克/千克/天口服完全防止病毒血症和死亡率。在进行这些研究时,没有证据表明血液学或临床化学方面存在神经毒性或异常。低至每天0.2毫克/千克的剂量是有效的；然而,低剂量时出现突破性病毒血症[2]。
[参考文献]
索立夫定物理化学性质
[ 密度 ]:
1.979g/cm3
[ 熔点 ]:
182 °C
[ 分子式 ]:
C11H13BrN2O6
[ 分子量 ]:
349.13500
[ 精确质量 ]:
347.99600
[ PSA ]:
124.78000
[ 折射率 ]:
1.746
[ 储存条件 ]:
2-8°C
索立夫定毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- UV9009810
- CHEMICAL NAME :
- 2,4(1H,3H)-Pyrimidinedione, 1-beta-D-arabinofuranosyl-5-(2-bromoethenyl)-, (E)-
- CAS REGISTRY NUMBER :
- 77181-69-2
- LAST UPDATED :
- 199503
- DATA ITEMS CITED :
- 15
- MOLECULAR FORMULA :
- C11-H13-Br-N2-O6
- MOLECULAR WEIGHT :
- 349.17
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >8 gm/kg
- TOXIC EFFECTS :
- Gastrointestinal - other changes
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >2 gm/kg
- TOXIC EFFECTS :
- Behavioral - altered sleep time (including change in righting reflex) Kidney, Ureter, Bladder - other changes in urine composition
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >2 gm/kg
- TOXIC EFFECTS :
- Behavioral - altered sleep time (including change in righting reflex) Kidney, Ureter, Bladder - other changes in urine composition
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- >10 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- >3 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- >5 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- >5 gm/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 72800 mg/kg/26W-C
- TOXIC EFFECTS :
- Liver - other changes Endocrine - hyperglycemia Blood - changes in cell count (unspecified)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 112 gm/kg/4W-I
- TOXIC EFFECTS :
- Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 45 gm/kg/4W-C
- TOXIC EFFECTS :
- Cardiac - EKG changes not diagnostic of specified effects
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 182 gm/kg/26W-C
- TOXIC EFFECTS :
- Endocrine - other changes Blood - changes in spleen Related to Chronic Data - death
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 22 gm/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Specific Developmental Abnormalities - other developmental abnormalities
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 500 mg/kg
- SEX/DURATION :
- female 17-20 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - live birth index (measured after birth)
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 1625 mg/kg
- SEX/DURATION :
- female 6-18 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
- TYPE OF TEST :
- Sister chromatid exchange
- TEST SYSTEM :
- Human Lymphocyte
- DOSE/DURATION :
- 200 mg/L
- REFERENCE :
- LIFSAK Life Sciences. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1-8, 1962-69; V.14- 1974- Volume(issue)/page/year: 38,281,1986
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区域：上海市浦东新区
价格：
￥需询单/1g
联系人：赖经理
产品详情：Sorivudine
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区域：上海市嘉定区
价格：
￥4297.0/50mg
联系人：夏言
产品详情：[Perfemiker]索立夫定,95%
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区域：上海市浦东新区
价格：
￥3351.0/50mg
￥需询单/1g
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￥需询单/1g
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产品详情：Sorivudine
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