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Delavirdine (Synonyms: 地拉韦啶; U 90152; BHAP-U 90152)
Delavirdine (U 90152) 是一种有效的口服活性非核苷逆转录酶抑制剂 (NNRTI)。Delavirdine 选择性地抑制 HIV-1 逆转录酶 (HIV-1 RT) (IC50=0.26 μM)，选择性超过 DNA 聚合酶 α (IC50=440 μM) 和 DNA 聚合酶 δ (IC50>550 μM)。Delavirdine 是HIV-1 病毒复制的抑制剂，可以用于艾滋病的相关研究。
Delavirdine Chemical Structure
CAS No. : 136817-59-9
| 规格 | 是否有货 | ||
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| 5 mg | 询价 | ||
| 10 mg | 询价 | ||
| 25 mg | 询价 |
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| 生物活性 |
Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs[1]. |
IC50 & Target |
IC50: 0.26 μM (HIV-1 RT); 440 μM (DNA polymerase α); >550 μM (DNA polymerase δ)[1] |
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| 体外研究 (In Vitro) |
Delavirdine has an 50% cytotoxicity at concentrations >100 μM in H9 and PBMC cultures.Delavirdine has low cellular cytotoxicity, causing less than 8% reduction in peripheral blood lymphocyte viability at 100 μM[1]. Delavirdine inhibits HIV-1 reverse transcriptase (RT) wild type with an IC50 value of 0.26 μM, and it inhibits Y181C-substituted RT and K103N-substituted RT with IC50 values of 8.32 uM and 7.7 uM, respectively[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
| 体内研究 (In Vivo) |
Delavirdine (U 90152) (oral gavage; 10 mg/kg, 200 mg/kg, 250 mg/kg; single dose) is absorbed and metabolized rapidly, that it constitutes a minor component in circulation, that its pharmacokinetics are nonlinear, and that its metabolism to desalkyl delavirdine is capacity limited or inhibitable in CD-1 mice (PK study)[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
| Clinical Trial |
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| 分子量 |
456.56 |
| Formula |
C22H28N6O3S |
| CAS 号 |
136817-59-9 |
| 中文名称 |
地拉韦啶；地来夸明；地拉韦定；地拉夫定；地拉呋定 |
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
| 纯度 & 产品资料 |
Data Sheet (535 KB) 产品使用指南 (1538 KB)
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| 参考文献 |
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