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Bevirimat

Cat. No. M1865
Bevirimat Structure
Synonym:

BVM, MPC-4326, PA-457

Size Price Availability Quantity
5mg USD 225  USD250 In stock
10mg USD 360  USD400 In stock
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Quality Control
Biological Activity

Bevirimat, the prototype Human Immunodeficiency Virus type 1 (HIV-1) maturation inhibitor, is highly potent in cell culture and efficacious in HIV-1 infected patients. Maturation inhibitors are an experimental class of antiretrovirals that inhibit Human Immunodeficiency Virus (HIV) particle maturation, the structural rearrangement required to form infectious virus particles. Unlike protease inhibitors, Bevirimat (BVM) blocks the cleavage of the Gag capsid precursor (CA-SP1) to mature capsid (CA) protein, resulting in the release of immature, noninfectious viral particles. Bevirimat specifically inhibits a single cleavage event, the final processing step for the Gag precursor where p25 (CA-SP1) is cleaved to p24 (CA) and SP1. The protease-dependent bevirimat resistance and replication levels can be explained by differences in CA/p2 cleavage processing by the different proteases.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 584.82
Formula C36H56O6
CAS Number 174022-42-5
Purity >99%
Solubility DMSO 10 mM
Storage at -20°C
References

Synthesis of betulinic acid derivatives as entry inhibitors against HIV-1 and bevirimat-resistant HIV-1 variants.
Dang et al. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5190-4. PMID: 22818973.

The prototype HIV-1 maturation inhibitor, bevirimat, binds to the CA-SP1 cleavage site in immature Gag particles.
Nguyen et al. Retrovirology. 2011 Dec 7;8:101. PMID: 22151792.

Improved Bevirimat resistance prediction by combination of structural and sequence-based classifiers.
Dybowski et al. BioData Min. 2011 Nov 14;4:26. PMID: 22082002.

HIV-1 protease inhibitor mutations affect the development of HIV-1 resistance to the maturation inhibitor bevirimat.
Fun et al. Retrovirology. 2011 Aug 24;8:70. PMID: 21864346.

A single polymorphism in HIV-1 subtype C SP1 is sufficient to confer natural resistance to the maturation inhibitor bevirimat.
Lu et al. Antimicrob Agents Chemother. 2011 Jul;55(7):3324-9. PMID: 21502630.

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Keywords: Bevirimat, BVM, MPC-4326, PA-457 supplier, HIV Protease, inhibitors

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