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Fosamprenavir sodium  (Synonyms: Amprenavir phosphate sodium; GW 433908 sodium)

目录号: HY-78726A
产品使用指南 技术支持

Fosamprenavir sodium 是一种口服有效、靶向 HIV-1 蛋白酶的抑制剂,是 Amprenavir (HY-17430) 的前药。Fosamprenavir sodium 在肠道上皮经细胞磷酸酶水解为 Amprenavir (VX-478),Amprenavir 通过与 HIV-1 蛋白酶的活性位点结合,阻止病毒 gag 和 gag-pol 多蛋白前体的加工,从而抑制成熟感染性病毒颗粒的形成,发挥抗 HIV-1 感染的活性。Fosamprenavir sodium 可用于人类免疫缺陷病毒 (HIV-1) 感染的研究。

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Fosamprenavir sodium

Fosamprenavir sodium Chemical Structure

CAS No. : 226700-80-7

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Fosamprenavir sodium 的其他形式现货产品:

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  • 生物活性

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生物活性

Fosamprenavir sodium is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir sodium is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir sodium can be used for the study of human immunodeficiency virus (HIV-1) infection[1][2].

IC50 & Target

HIV-1

 

体外研究
(In Vitro)

Fosamprenavir sodium 的活性形式 Amprenavir 在体外实验中可结合并抑制 pepsin 的活性,IC50 为 3.56 μM[2]

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

体内研究
(In Vivo)

Fosamprenavir (20 mg/kg/天;灌胃;每日;4 周) sodium 在 Jackson A/J 小鼠的喉咽反流模型中,可防止胃蛋白酶介导的喉损伤 (如反应性上皮、上皮内炎症细胞增加和细胞凋亡)[2]

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

Animal Model: 6-week-old female Jackson A/J mice with laryngopharyngeal reflux model (mechanical laryngeal injury once weekly for 2 weeks and pH7 solvent/pepsin instillation 3 days/week for 4 weeks)[2]
Dosage: 20 mg/kg/day Fosamprenavir
Administration: gavage, daily, 4 weeks (5 days/week)
Result: Prevented pepsin-mediated laryngeal damage, which was characterized by reactive epithelia, increased intraepithelial inflammatory cells, and cell apoptosis.
Clinical Trial
分子量

629.57

Formula

C25H34N3Na2O9PS

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
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  • 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 *
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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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Fosamprenavir sodium
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HY-78726A
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