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BMS-663068

Cat. No. M2463
BMS-663068 Structure
Synonym:

Fostemsavir

Size Price Availability Quantity
5mg USD 230  USD230 In stock
25mg USD 700  USD700 In stock
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Quality Control & Documentation
Biological Activity

BMS-663068 is the phosphonooxymethyl prodrug of BMS626529, a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells with EC50 of < 10 nM.

Chemical Information
Molecular Weight 583.49
Formula C25H26N7O8P
CAS Number 864953-29-7
Solubility (25°C) DMSO 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Michael Kozal, et al. Fostemsavir in Adults with Multidrug-Resistant HIV-1 Infection

[2] Mary C Cambou, et al. Novel Antiretroviral Agents

[3] Ester Ballana, et al. BMS-663068, a safe and effective HIV-1 attachment inhibitor

[4] Cynthia Brinson, et al. HIV-1 attachment inhibitor prodrug BMS-663068 in antiretroviral-experienced subjects: week 24 sub-group analysis

[5] Zhufang Li, et al. Activity of the HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068, against CD4-independent viruses and HIV-1 envelopes resistant to other entry inhibitors

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Keywords: BMS-663068, Fostemsavir supplier, HIV Protease, inhibitors, activators


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