1. Anti-infection
  2. HIV Reverse Transcriptase
  3. HIV-1 inhibitor-49

HIV-1 inhibitor-49 是一种口服有效的 HIV-1 抑制剂,是一种 HEPT 类似物。HIV-1 inhibitor-49 具有良好的药代动力学特征和有效的非核苷类逆转录酶 (Reverse Transcriptase; IC50=30 nM) 抑制活性。HIV-1 inhibitor-49 具有潜在的安全性,对小鼠无急性毒性。

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HIV-1 inhibitor-49 Chemical Structure

HIV-1 inhibitor-49 Chemical Structure

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Customer Review

查看 HIV 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model[1].

IC50 & Target[1]

HIV-1 (WT)

17 nM (EC50)

HIV-1 (L100I)

0.38 μM (EC50)

HIV-1 (K103N)

2.64 μM (EC50)

HIV-1 (Y181C)

1.85 μM (EC50)

HIV-1 (E138K)

0.09 μM (EC50)

体外研究
(In Vitro)

HIV-1 inhibitor-49 (化合物 9h) (EC50=17 nM-39.21 μM) 抑制 WT HIV-1,其选择性指数远高于对其他 HIV-1 突变体 (L100I, K103N, Y181C和E138K)[1]
HIV-1 inhibitor-49 (0-50 μM) 在 CHO-hERG 细胞中对 CYP2C9CYP2C19 的 IC50 分别为 27.6 μM (CYP2C9)和30.3 μM (CYP2C19),而对其他 CYP 的抑制效力 >50 μM,对 hERG 的抑制效力 >40 μM[1]

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

体内研究
(In Vivo)

HIV-1 inhibitor-49 (化合物 9h) (1000mg /kg; 灌胃; 单剂量) 在健康小鼠模型中无明显的病理损伤和死亡诱导倾向[1]
HIV-1 inhibitor-49 (10 mg/kg; 口服; 单剂量) 在大鼠中表现出良好的口服生物利用度[1]

大鼠中的药代动力谱[1]

Route Dose (mg/kg) AUC0-t (ng·h/mL) AUC0-∞ (ng·h/mL) T1/2 (h) Tmax (h) Vz (mL/kg) Cl (mL/h/kg) Cmax (ng/mL) F (%)
i.v. 1.0 1102 1100 0.514 0.083 698 936 2033
p.o. 10 9557 8663 2.51 0.583 3523 86.72%

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

分子量

416.44

Formula

C21H18F2N2O3S

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-49 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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产品名称:
HIV-1 inhibitor-49
目录号:
HY-151933
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