索立夫定
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- CAS号:
- 77181-69-2
- 英文名:
- sorivudine
- 英文别名:
- YN-72;BvAraU;D01734;BV-araU;Bravavir;Brovavir;Sorivudin;sorivudine;Bravavir (tn);Sorivudine (jan/usan/inn)
- 中文名:
- 索立夫定
- 中文别名:
- 索立夫定;化合物 T16911;1-BETA-D-阿拉伯糖呋喃糖基-5-[(1E)-2-溴乙烯基]-2,4(1H,3H)-嘧啶二酮
- CBNumber:
- CB51074625
- 分子式:
- C11H13BrN2O6
- 分子量:
- 349.13
- MOL File:
- 77181-69-2.mol
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索立夫定化学性质
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熔点:
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182° (Sakata, 1980); mp 195-200° (dec) (Machida, Sakata, 1983)
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比旋光度:
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D25 +0.5° (1N NaOH)
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密度:
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1.979±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: 250 mg/mL (716.07 mM)
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酸度系数(pKa):
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8.37±0.10(Predicted)
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索立夫定性质、用途与生产工艺
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)。
Sorivudine (BV-araU) inhibits strains of HSV-1 and HSV-2 (wild-type strains VR-3 and UW-268) with ID
50
s (50% inhibitory dose) of 0.39 and 0.67 μM, respectively.
Sorivudine has antiviral activity against several viruses including varicella zoster virus, herpes simplex type 1 virus, and Epstein-Barr virus.
Sorivudine (BV-araU) is a pyrimidine nucleoside analog which has in vitro inhibitory activity against varicella zoster virus (VZV) at concentrations of 00001-0.004 mg/ml These concentrations are over 1000-fold lower than those which are required for the inhibition of VZV replication by acyclovir 3 Sorivudine also inhibits HSV-I replication at concentrations ranging from 0.03-0.1 mg/ml.
Sorivudine (BV-araU) has been evaluated in the treatment of HSV-l encephalitis when administered orally to mice. At dosages in excess of 12.5 mg/kg, survival of treated mice is prolonged. With doses in excess of 50 mg/kg, a significant decrease in mortality was achieved as we1l. A more relevant model is that of simian varicella virus infection in African green monkeys (Cerophithecus aethiops). In this system, Sorivudine therapy at dosages as low as 20 mg/kg per day given intramuscularly or 100 mg/kg per day administered orally completely protected against viremia and mortality. In the conduct of these studies, there was no evidence of neurotoxicity or abnormalities in hematology or clinical chemistries. Doses as low as 0.2 mg/kg per day were effective; however, breakthrough viremia was noted at lower dosages.
索立夫定
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-123032 | Sorivudine | | 1 mg | 552元 |
| 2023/03/20 | HY-123032 | 索立夫定
Sorivudine | 77181-69-2 | 5mg | 1450元 |
77181-69-2, 索立夫定 相关搜索:
- C11H13BrN2O6
- 化合物 T16911
- 1-BETA-D-阿拉伯糖呋喃糖基-5-[(1E)-2-溴乙烯基]-2,4(1H,3H)-嘧啶二酮
- 索立夫定
- 77181-69-2
- 1-β-D-Arabinofuranosyl-5-[(1E)-2-bromoethenyl]-2,4(1H,3H)-pyrimidinedione
- nucleoside,antiviral,inhibit,antimetabolite,Epstein-Barr,pyrimidine,virus,zoster,oral,varicella,Sorivudine,Inhibitor,herpes,DNA/RNA Synthesis,simplex,type
- 2,4(1H,3H)-Pyrimidinedione, 1-β-D-arabinofuranosyl-5-[(1E)-2-bromoethenyl]-
- 1-β-D-Arabinofuranosyl-5-[(1E)-2-bromoethenyl]-2,4(1H,3H)-pyrimidinedione
- Sorivudin
- Sorivudine (jan/usan/inn)
- D01734
- Bravavir (tn)
- Bravavir
- YN-72
- BV-araU
- BvAraU
- Brovavir
- 1-β-D-Arabinofuranosyl-5-[(E)-2-bromovinyl]-1,2,3,4-tetrahydropyrimidine-2,4-dione
- 1-(β-D-Arabinofuranosyl)-5-[(E)-2-bromoethenyl]uracil
- sorivudine