TAK-220
TAK-220(TAK-220)
CAS: 333994-00-6
化学式: C31H41ClN4O3
| 中文名 | TAK-220 |
| 英文名 | TAK-220 |
| 别名 | 化合物 T16973 |
| 英文别名 | TAK220 TAK-220 TAK 220 1-ACETYL-N-(3-(4-(4-CARBAMOYLBENZYL)PIPERIDIN-1-YL)PROPYL)-N-(3-CHLORO-4-METHYLPHENYL)PIPERIDINE-4-CARBOXAMIDE 4-Piperidinecarboxamide, 1-acetyl-N-[3-[4-[[4-(aminocarbonyl)phenyl]methyl]-1-piperidinyl]propyl]-N-(3-chloro-4-methylphenyl)- |
| CAS | 333994-00-6 |
| 化学式 | C31H41ClN4O3 |
| 分子量 | 553.14 |
| 密度 | 1.208±0.06 g/cm3(Predicted) |
| 熔点 | 166-167 °C(Solv: ethyl acetate (141-78-6); ethanol (64-17-5)) |
| 沸点 | 757.8±60.0 °C(Predicted) |
| 溶解度 | 10毫米DMSO |
| 酸度系数 | 16.16±0.50(Predicted) |
| 存储条件 | -20℃ |
| 体外研究 | TAK-220 is a selective CCR5 antagonist, with IC 50 s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5 in CHO cells, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7. TAK-220 (0-1000 nM) interacts with CCR5 but not with RANTES and inhibits the CCR5-mediated Casup>2+ signaling. TAK-220 inhibits R5 HIV-1 (JR-FL) envelope-mediated membrane fusion, with an IC 50 value of 0.42 nM, but does not alter X4 HIV-1 (HXB2) envelope-mediated membrane fusion. TAK-220 also selectively inhibits HIV-1, with EC 50 s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC 90 s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs. TAK-220 shows potent inhibitory activity against the R5 isolates, with IC 50 s of 3.12 nM against HIV-1 R5-08, 13.47 nM against HIV-1 R5-06, and 2.26 nM against HIV-1 R5-18. TAK-220 (>100 nM) has no toxicity in uninfected PBMCs. |
TAK-220 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.808 ml | 9.039 ml | 18.079 ml |
| 5 mM | 0.362 ml | 1.808 ml | 3.616 ml |
| 10 mM | 0.181 ml | 0.904 ml | 1.808 ml |
| 5 mM | 0.036 ml | 0.181 ml | 0.362 ml |
最后更新：2024-01-02 23:10:35
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