1. Anti-infection
  2. HIV Reverse Transcriptase
  3. HIV-1 inhibitor-50

HIV-1 inhibitor-50 是一种非核苷逆转录酶抑制剂 (NNRTI),靶向 HIV-1 逆转录酶 (RT) (IC50=50 nM)。HIV-1 inhibitor-50 具有显著的抗病毒活性,对 HIV-1 IIIB 及其突变株的 EC50 为 2.22-53.3 nM。

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HIV-1 inhibitor-50 Chemical Structure

HIV-1 inhibitor-50 Chemical Structure

CAS No. : 2834087-69-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HIV-1 invistor-50 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that targets HIV-1 reverse transcriptase (RT) (IC50=50 nM). HIV-1 inhibitor-50 shows significant antiviral activity, with EC50s of 2.22-53.3nM against HIV-1 IIIB and its mutant strains[1].

IC50 & Target[1]

HIV-1 (WT)

3.04 nM (EC50)

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)

体外研究
(In Vitro)

HIV-1 inhibitor-50 (化合物 36a) 保护 MT-4 细胞免受 HIV-1 IIIB 和 RES056 的侵袭,EC50 分别为 2.22 nM 和 53.3 nM[1]
HIV-1 inhibitor-50 抑制 MT-4 细胞活力,CC50 为 45.6 μM[1]
HIV-1 inhibitor-50 在微粒体和肝脏中具有较低的内在清除率 (CLs 分别为 87.6 μL/min/mg 和 16.6 μL/min/mg),并具有较高的代谢稳定性 (T1/2=11.3 min)[1]

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

Cell Viability Assay[1]

Cell Line: MT-4 cells
Concentration:
Incubation Time:
Result: Inhibited HIV-1 infection in MT-4 cells with EC50 values of 3.04 nM (L100I), 2.87 nM (K103N), 10.2 nM (Y181C), 13.2 nM (Y188L), 9.77 nM (E138K), 19.8 nM (F227L+V106A), respectively.
体内研究
(In Vivo)

HIV-1 inhibitor-50 (化合物 36a) (盐酸盐形式; 2 mg/kg; 静脉注射; 单剂量) 具有较高的清除率 (CL=103 L/h/kg) 和适度的半衰期 (T1/2=1.43 h)[1]
HIV-1 inhibitor-50 (盐酸盐形式; 2000 mg/kg; 口服给药; 单剂量) 在 7 天内与对照组相比没有引起任何异常行为或显著的体重变化,表明没有急性毒性[1]

药代动力学分析[1]

Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (h·ng/mL) AUC0-∞ (h·ng/mL) CL (L/h/kg) F (%)
i.v. 2 1.43 0 484 250 255 103 /
p.o. 10 5.12 0.25 37.5 107 154 / 12.1

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

分子量

427.43

Formula

C24H18FN5O2

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-50 相关分类

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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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HIV-1 inhibitor-50
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HY-152160
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