FESTINAVIR
| 中文名称 | FESTINAVIR |
|---|---|
| 中文同义词 | 化合物 T30791;2′,3′-二脱氢-3′-脱氧-4′-乙炔基胸苷 |
| 英文名称 | Censavudine |
| 英文同义词 | 2',3'-Didehydro-3'-deoxy-4'-ethynylthymidine;4'-Ed4T;BMS 986001;Censavudine;Festinavir;Thymidine, 2',3'-didehydro-3'-deoxy-4'-ethynyl-;OBP 601;OBP601 |
| CAS号 | 634907-30-5 |
| 分子式 | C12H12N2O4 |
| 分子量 | 248.23 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 634907-30-5.mol |
| 结构式 |  |
FESTINAVIR 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；需要超声波） |
| 酸度系数(pKa) | 9.47±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
|
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-16776 | Censavudine | 1 mg | 2480元 | |
| 2024/08/19 | HY-16776 | FESTINAVIR Censavudine | 634907-30-5 | 5 mg | 6200元 |