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Brecanavir

Cat. No. M29893
Brecanavir Structure
Synonym:

GW640385

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Biological Activity

Brecanavir (GW640385) is a novel, potent HIV protease inhibitor.

Chemical Information
Molecular Weight 703.82
Formula C33H41N3O10S2
CAS Number 313682-08-5
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] Emile J Velthuisen, et al. Eur J Med Chem. Synthesis and pharmacokinetic profile of highly deuterated brecanavir analogs

[2] Richard Hazen, et al. Antimicrob Agents Chemother. In vitro antiviral activity of the novel, tyrosyl-based human immunodeficiency virus (HIV) type 1 protease inhibitor brecanavir (GW640385) in combination with other antiretrovirals and against a panel of protease inhibitor-resistant HIV

[3] No authors listed. AIDS Patient Care STDS. Brecanavir's hopes dashed

[4] Y Sunila Reddy, et al. Antimicrob Agents Chemother. Safety and pharmacokinetics of brecanavir, a novel human immunodeficiency virus type 1 protease inhibitor, following repeat administration with and without ritonavir in healthy adult subjects

[5] Susan L Ford, et al. Antimicrob Agents Chemother. Single-dose safety and pharmacokinetics of brecanavir, a novel human immunodeficiency virus protease inhibitor

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Keywords: Brecanavir, GW640385 supplier, HIV Protease, inhibitors, activators


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