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

Aplaviroc (Synonyms: AK 602; GSK 873140; GW 873140; ONO 4128)

Cat. No.: HY-17450
Handling Instructions

Aplaviroc, 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

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  • Biological Activity

  • Technical Information

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  • References

Description

Aplaviroc, 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 (AK602) is identified as the most potent agent among newly designed and synthesized SDP derivatives. 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. It is of note that Aplaviroc is substantially more potent than two previously published CCR5 inhibitors, E921/TAK-779 and AK671/SCH-C. The activity of Aplaviroc’s anti-HIV-1 is limited and similar to that seen for zidovudine. Moreover, 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), while these two R5 HIV-1 variants are less susceptible to zidovudine, nelfinavir, and saquinavir. 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7310 mL 8.6549 mL 17.3097 mL
5 mM 0.3462 mL 1.7310 mL 3.4619 mL
10 mM 0.1731 mL 0.8655 mL 1.7310 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

577.71

Formula

C₃₃H₄₃N₃O₆

CAS No.

461443-59-4

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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Aplaviroc
Cat. No.:
HY-17450
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Aplaviroc

Cat. No.: HY-17450