上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物,专注于信号通路和疾病研究领域。
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
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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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