1. Anti-infection
  2. HIV Reverse Transcriptase
  3. HIV-1 inhibitor-51

HIV-1 inhibitor-51 是一种非核苷逆转录酶抑制剂 (NNRTI),对 WT HIV-1 (IIIB) 和一组突变株表现出出色的抗病毒活性。HIV-1 inhibitor-51 对 WT HIV-1 RT 具有高结合亲和力 (KD=2.50 μM) 和抑制活性 (IC50=0.03 μM)。HIV-1 inhibitor-51 对突变株 (L100I、K103N、Y181C、Y188L、E138K、F227L + V106A、RES056) 的 EC50 为 2.22-53.3 nM。

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HIV-1 inhibitor-51 Chemical Structure

HIV-1 inhibitor-51 Chemical Structure

CAS No. : 2834087-82-8

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生物活性

HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056)[1].

IC50 & Target[1]

HIV-1 (WT)

0.03 μM (IC50)

HIV-1 (WT)

2.5 μM (Kd)

HIV-1 (L100I)

3.04 nM (EC50)

HIV-1 (K103N)

2.87 nM (EC50)

HIV-1 (Y181C)

10.2 nM (EC50)

HIV-1 (Y188L)

13.2 nM (EC50)

HIV-1 (E138K)

9.77 nM (EC50)

HIV-1 (F227L+V106A)

19.8 nM (EC50)

HIV-1 (RES056)

53.3 nM (EC50)

体内研究
(In Vivo)

HIV-1 inhibitor-51 (化合物 36a·HCl; 2 mg/kg; 静脉给药) 的 T1/2 为 1.43 小时,CL 为 103 L/h·kg,Cmax 为 484 ng/mL[1]
HIV-1 inhibitor-51 (10 mg/kg; 口服) 的 T1/2 为 5.12 小时,Cmax 为 37.5 ng/mL[1]

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

Animal Model: ICR mice[1]
Dosage: 2 mg/kg (Pharmacokinetic Analysis)
Administration: IV
Result: Had a T1/2 of 5.12 hours, and Cmax of 37.5 ng/mL.
分子量

463.89

Formula

C24H19ClFN5O2

CAS 号
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

HIV-1 inhibitor-51 相关分类

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  • 稀释计算器

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

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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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产品名称:
HIV-1 inhibitor-51
目录号:
HY-152161
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