1. Anti-infection
  2. HIV Reverse Transcriptase
  3. Delavirdine

Delavirdine  (Synonyms: 地拉韦啶; U 90152; BHAP-U 90152)

目录号: HY-10571
产品使用指南

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。

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Delavirdine Chemical Structure

Delavirdine Chemical Structure

CAS No. : 136817-59-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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]

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].

MCE 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

456.56

Formula

C22H28N6O3S

CAS 号
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
参考文献

Delavirdine 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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