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Aplaviroc

Cat. No. M30120
Aplaviroc Structure
Synonym:

AK 602; GSK 873140; GW 873140

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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 577.71
Formula C33H43N3O6
CAS Number 461443-59-4
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Olga Latinovic, et al. Antiviral Res. Rapamycin enhances aplaviroc anti-HIV activity: implications for the clinical development of novel CCR5 antagonists

[2] Kathryn M Kitrinos, et al. Antimicrob Agents Chemother. Virologic failure in therapy-naive subjects on aplaviroc plus lopinavir-ritonavir: detection of aplaviroc resistance requires clonal analysis of envelope

[3] W G Nichols, et al. Antimicrob Agents Chemother. Hepatotoxicity observed in clinical trials of aplaviroc (GW873140)

[4] Brendan M Johnson, et al. J Clin Pharmacol. Evaluation of the drug interaction potential of aplaviroc, a novel human immunodeficiency virus entry inhibitor, using a modified cooperstown 5 + 1 cocktail

[5] Charlene Crabb. AIDS. GlaxoSmithKline ends aplaviroc trials

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Keywords: Aplaviroc, AK 602; GSK 873140; GW 873140 supplier, CCR, inhibitors, activators


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