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634907-30-5

中文名称 FESTINAVIR
英文名称 Censavudine
CAS 634907-30-5
分子式 C12H12N2O4
分子量 248.23
MOL 文件 634907-30-5.mol
更新日期 2025/09/10 14:47:31
634907-30-5 结构式 634907-30-5 结构式

基本信息

中文别名
化合物 T30791
英文别名
4'-Ed4T
BMS 986001
Festinavir
Censavudine
2',3'-Didehydro-3'-deoxy-4'-ethynylthymidine
Thymidine, 2',3'-didehydro-3'-deoxy-4'-ethynyl-
所属类别
生物化工:抑制剂

物理化学性质

熔点207-209℃
密度1.42±0.1 g/cm3(Predicted)
储存条件4°C, away from moisture
溶解度DMSO : 52 mg/mL (209.48 mM; Need ultrasonic)
酸度系数(pKa)9.47±0.10(Predicted)
形态Solid
颜色Light yellow to yellow
InChIInChI=1S/C12H12N2O4/c1-3-12(7-15)5-4-9(18-12)14-6-8(2)10(16)13-11(14)17/h1,4-6,9,15H,7H2,2H3,(H,13,16,17)/t9-,12+/m1/s1
InChIKeyOSYWBJSVKUFFSU-SKDRFNHKSA-N
SMILESOC[C@@]1(C#C)O[C@@H](N2C=C(C)C(=O)NC2=O)C=C1

安全数据

危险性符号(GHS)GHS hazard pictograms
GHS08
警示词警告
危险性描述H373-H341
FESTINAVIR价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-16776Censavudine634907-30-51 mg1670元
2025/05/22HY-16776FESTINAVIR
Censavudine
634907-30-55 mg3680元
2025/05/22HY-16776FESTINAVIR
Censavudine
634907-30-510 mM * 1 mLin DMSO4560元

常见问题列表

生物活性
Censavudine (OBP-601; BMS-986001),一种核苷类似物,是一种核苷逆转录酶 (nucleoside reverse transcriptase) 抑制剂。Censavudine 是一种有效的 HIV 抑制剂,对 HIV-2 和 HIV-1 的 EC50 范围分别为 30-81 nM 和 450-890 nM。
靶点

HIV-2

30-81 nM (EC 50 )

HIV-1

450-890 nM (IC 50 )

体外研究

BMS-986001 shows greater activity against HIV-2 ROD9 than against HIV-1 NL4-3 ; the mean EC 50 s for BMS-986001 are 74 nM for HIV-2 ROD9 and 890 nM for HIV-1 NL4-3 in the single-cycle assay. HIV-2 ROD9 also showes greater sensitivity to BMS-986001 in 4-day infections of an immortalized T cell line (CEMss), with the mean EC 50 for HIV-2 ROD9 (EC 50 of 0.14 nM) being 30-fold lower than that for HIV-1 NL4-3 (EC 50 of 4.2 nM).
BMS-986001 also exhibits full activity against HIV-2 variants whose genomes encoded the single amino acid changes K65R and Q151M in reverse transcriptase.

体内研究

The pharmacokinetic parameters of Censavudine (BMS-986001; 100-750 mg/kg) generated from the dried blood spot (DBS) assay and the plasma assay is compared. The ratios of the AUC (0-24 h) and C max for BMS-986001 in DBS compared to those in plasma are consistent at 0.83-0.91 and 0.81-0.97, respectively, across all dose groups in rats. The T max in rat DBS and plasma are also consistent at about 1 h.

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