1. Anti-infection
  2. Reverse Transcriptase HIV
  3. NNRT-IN-13

NNRT-IN-13 是一种强效的非核苷类逆转录酶 (NNRT) 抑制剂,可直接抑制 HIV-1 逆转录酶 (IC₅₀ = 0.25 μM)。NNRT-IN-13 对野生型 HIV-1 (EC₅₀ = 0.0046 μM) 及一系列耐药突变株均表现出优异的抗病毒活性。NNRT-IN-13 具有良好的体内代谢和安全性。NNRT-IN-13 可用于艾滋病 (HIV) 的相关研究。

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NNRT-IN-13

NNRT-IN-13 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

NNRT-IN-13 is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor that directly inhibiting HIV-1 reverse transcriptase (IC₅₀ = 0.25 μM). NNRT-IN-13 exhibits excellent antiviral activity against wild-type HIV-1 (EC₅₀ = 0.0046 μM) and a broad spectrum of drug-resistant mutants. NNRT-IN-13 exhibits favorable in vivo metabolic and safety profiles. NNRT-IN-13 can be used for human immunodeficiency virus (HIV) research[1].

体外研究
(In Vitro)

NNRT-IN-13 (compound 15k) 对野生型 HIV-1 表现出优异的抗病毒活性 (EC₅₀ = 0.0046 μM),并对一系列耐药突变株具有广谱活性,包括 L100I (0.0053 μM)、K103N (0.0034 μM)、Y181C (0.010 μM)、Y188L (0.026 μM)、E138K (0.015 μM)、F227L/V106A (0.033 μM) 以及 K103N/Y181C (0.029 μM),同时在 MT-4 细胞中显示出较低的细胞毒性 (CC₅₀ = 26.64 μM)[1]
NNRT-IN-13 以独特的 “Y” 形模式与 HIV-1 逆转录酶结合,并与 p51-p66 界面残基 E138 和 K101 形成新型氢键[1]
NNRT-IN-13 对 CYP1A2、CYP2C9、CYP2C19 和 CYP2D6 无抑制作用 (IC₅₀ 值均大于 50 μM),并且对 CYP3A4 仅表现出微弱的抑制 (IC₅₀ = 13.6 μM)[1]

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

体内研究
(In Vivo)

NNRT-IN-13 (50 与 2000 mg/kg,腹腔注射,单次给药或隔日给药持续 14 天) 在昆明小鼠体内未表现出毒性反应,且未引起器官损伤[1]

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

Animal Model: Kunming mice[1]
Dosage: 2000 mg/kg
Administration: i.p., single dose
Result: Showed no mortality or adverse toxicity signs, including anorexia, lethargy, alopecia, or dyspnea.
Exhibited steady weight gain over the seven-day observation period, with no significant differences compared to control.
Animal Model: Kunming mice[1]
Dosage: 50 mg/kg
Administration: i.p., every other day for 14 days
Result: Showed no apparent toxicity signs or behavioral abnormalities (such as lethargy, clonic convulsions, anorexia, and ruffled fur.
Gained normal body weight and were equivalent to those of the control group.
Exhibited no visible pathological changes or lesions were detected in the heart, liver, spleen, lungs, or kidneys.
分子量

614.72

Formula

C31H34N8O4S

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
  • 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:
NNRT-IN-13
目录号:
HY-178341
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