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

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

Cat. No.: HY-17450
Handling Instructions

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.

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

Aplaviroc Chemical Structure

Aplaviroc Chemical Structure

CAS No. : 461443-59-4

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other In-stock Forms of Aplaviroc:

Other Forms of Aplaviroc:

Top Publications Citing Use of Products

View All CCR Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

 

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

577.71

Formula

C₃₃H₄₃N₃O₆

CAS No.
SMILES

O=C(O)C1=CC=C(OC2=CC=C(CN(CC3)CCC3(N(CCCC)C([[email protected]@H]([[email protected]@H](C4CCCCC4)O)N5)=O)C5=O)C=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

AplavirocAK 602 GSK 873140 GW 873140AK602AK-602GSK873140GSK 873140GSK-873140GW873140GW 873140GW-873140CCRHIVCC chemokine receptorHuman immunodeficiency virusInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Aplaviroc
Cat. No.:
HY-17450
Quantity:
MCE Japan Authorized Agent: