1. GPCR/G Protein Immunology/Inflammation Anti-infection
  2. CCR HIV
  3. Aplaviroc

Aplaviroc  (Synonyms: AK 602; GSK 873140; GW 873140)

目录号: HY-17450
产品使用指南

Aplaviroc (AK 602),SDP的一个衍生物,是 CCR5 的拮抗剂,其对 HIV-1Ba-L, HIV-1JRFL 和 HIV-1MOKWIC50 值为 0.1-0.4 nM。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Aplaviroc hydrochloride 通常具有更好的水溶性和稳定性。

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Aplaviroc Chemical Structure

Aplaviroc Chemical Structure

CAS No. : 461443-59-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Aplaviroc (AK 602), a SDP derivative, is a CCR5 antagonist, with IC50s of 0.1-0.4 nM for HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW.

IC50 & Target[1]

HIV-1Ba-L

0.4 nM (IC50)

HIV-1JRFL

0.1 nM (IC50)

HIV-1MOKW

0.2 nM (IC50)

CCR5

 

体外研究
(In Vitro)

Aplaviroc exerts potent activity against three wild-type R5 HIV-1 strains (HIV-1Ba-L, HIV-1JRFL and HIV-1MOKW) with IC50 values of 0.1 to 0.4 nM. Aplaviroc is substantially more potent than two previously published CCR5 inhibitors, E921/TAK-779 and AK671/SCH-C. Aplaviroc suppresses the infectivity and replication of two HIV-1MDR variants, HIV-1MM and HIV-1JSL, at extremely low concentrations (IC50 values of 0.4 to 0.6 nM). Aplaviroc binds to CCR5 with high affinity. The Kd values thus determined for Aplaviroc, E913, E921/TAK-779, and AK671/SCH-C are 2.9±1.0, 111.7±3.5, 32.2±9.6, and 16.0±1.5 nM, respectively. Aplaviroc potently blocks rgp120/sCD4 binding to CCR5 with an IC50 value of 2.7 nM. These results suggest that the potent activity of Aplaviroc against R5 HIV-1 stems from its binding to ECL2B and/or its vicinity with high affinity, resulting in inhibition of gp120/CD4 binding to CCR5[1].

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

体内研究
(In Vivo)

The concentration of Aplaviroc (AK602) reached the maximal concentration immediately after intraperitoneal administration and decreased rapidly[2].
Aplaviroc (AK602, 60 mg/kg, bid, daily) suppresses R5 HIV-1 viremia in hu-PBMC-NOG mice[2].

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

Animal Model: hu-PBMC-NOG mice[2].
Dosage: 60 mg/kg.
Administration: Single intraperitoneal administration, bid, daily.
Result: The numbers of CD4+ cells/μL in saline-treated mice were significantly less than those of AK602-treated, ddI-treated, or uninfected mice.
Clinical Trial
分子量

577.71

Formula

C33H43N3O6

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
  • 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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