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

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

Cat. No.: HY-17450
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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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Aplaviroc hydrochloride) usually boasts enhanced water solubility and stability.

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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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].

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

Aplaviroc Related Antibodies
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].

MedChemExpress (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([C@@H]([C@@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.
Purity & Documentation
References
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Aplaviroc Related Classifications

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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.

Keywords:

Aplaviroc461443-59-4AK 602 GSK 873140 GW 873140AK602AK-602GSK873140GSK 873140GSK-873140GW873140GW 873140GW-873140CCRHIVCC chemokine receptorHuman immunodeficiency virusInhibitorinhibitorinhibit

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