634907-30-5
基本信息
BMS 986001
Festinavir
Censavudine
2',3'-Didehydro-3'-deoxy-4'-ethynylthymidine
Thymidine, 2',3'-didehydro-3'-deoxy-4'-ethynyl-
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 |
| InChI | InChI=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 |
| InChIKey | OSYWBJSVKUFFSU-SKDRFNHKSA-N |
| SMILES | OC[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) |  GHS08 |
| 警示词 | 警告 |
| 危险性描述 | H373-H341 |
| 防范说明 | P201-P202-P281-P308+P313-P405-P501-P260-P314-P501 |
常见问题列表
|
HIV-2 30-81 nM (EC 50 ) |
HIV-1 450-890 nM (IC 50 ) |
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.
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.