1. Metabolic Enzyme/Protease
  2. HIV Integrase
  3. HIV-1 integrase inhibitor 10

HIV-1 integrase inhibitor 10 是一种 HIV-1 变构整合酶抑制剂 (ALLINI),具有口服活性。HIV-1 integrase inhibitor 10 可抑制 NLRepRluc 病毒在 MT-2 细胞中的生长,其 EC50 值为 3-5 nM。HIV-1 integrase inhibitor 10 可用于人类免疫缺陷病毒-1 (HIV-1) 的研究。

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HIV-1 integrase inhibitor 10 Chemical Structure

HIV-1 integrase inhibitor 10 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HIV-1 integrase inhibitor 10 is an orally active HIV-1 allosteric integrase inhibitor (ALLINI). HIV-1 integrase inhibitor 10 can inhibit viral outgrowth of the NLRepRluc virus in MT-2 cells with EC50 values of 3-5 nM. HIV-1 integrase inhibitor 10 can be used for the research of Human immunodeficiency virus-1 (HIV-1)[1].

IC50 & Target

EC50 for NLRepRluc virus: 3.9 nM (T/T); 4.5 nM (N/A); 5.2 nM (A/A)[1].

体外研究
(In Vitro)

HIV-1 integrase inhibitor 10 (compound 11) has excellent antiviral potency for viruses containing the T/T, N/A and A/A polymorphs with EC50 values of 3.9 nM, 4.5 nM and 5.2 nM, respectively[1].

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

体内研究
(In Vivo)

HIV-1 integrase inhibitor 10 (compound 11) (1 mg/kg, iv. and 5 mg/kg, po., as solutions in 90:10 PEG-400:EtOH for IV dosing and 90:5:5 PEG-400:EtOH:TPGS for PO dosing) exhibits improved rat PK properties[1].

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

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 1 mg/kg, 5 mg/kg
Administration: 1 mg/kg, iv. and 5 mg/kg, po., as solutions in 90:10 PEG-400:EtOH for IV dosing and 90:5:5 PEG-400:EtOH:TPGS for PO dosing.
Result:
Compound Rat Cl (mL/min/kg) Rat AUC0-∞ (nMhr) Rat %F PAMPA permeability (nM/sec) at pH 5.5/7.4
HIV-1 integrase inhibitor 10 (Compound 11) 2.8 36,305 83% 1009/752
分子量

687.83

Formula

C40H45N7O4

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 integrase inhibitor 10 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 integrase inhibitor 10
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HY-150079
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