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

Aplaviroc hydrochloride (Synonyms: AK602 hydrochloride; GSK-873140 hydrochloride; GW-873140 hydrochloride)

Cat. No.: HY-17450A Purity: 99.76%
Handling Instructions

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

For research use only. We do not sell to patients.

Aplaviroc hydrochloride Chemical Structure

Aplaviroc hydrochloride Chemical Structure

CAS No. : 461023-63-2

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1 mg USD 580 In-stock
Estimated Time of Arrival: December 31
5 mg USD 950 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
25 mg USD 3450 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Aplaviroc (AK 602) hydrochloride, 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

HIV-1Ba-L

0.4 nM (IC50)

HIV-1JRFL

0.1 nM (IC50)

HIV-1MOKW

0.2 nM (IC50)

CCR5

 

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.

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
Molecular Weight

614.17

Formula

C₃₃H₄₄ClN₃O₆

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (325.64 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6282 mL 8.1411 mL 16.2821 mL
5 mM 0.3256 mL 1.6282 mL 3.2564 mL
10 mM 0.1628 mL 0.8141 mL 1.6282 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 12.5 mg/mL (20.35 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 12.5 mg/mL (20.35 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 12.5 mg/mL (20.35 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.76%

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Aplaviroc hydrochloride
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HY-17450A
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