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Censavudine

Cat. No. M30402
Censavudine Structure
Synonym:

OBP-601; BMS-986001; TPN-101

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Biological Activity

Censavudine (OBP-601; BMS-986001), a nucleoside analog, is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1, respectively.

Chemical Information
Molecular Weight 248.23
Formula C12H12N2O4
CAS Number 634907-30-5
Form Solid
Solubility (25°C) DMSO 52 mg/mL (ultrasonic)
Water 10 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 4°C, dry, sealed
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] Richard C Burrell, et al. J Labelled Comp Radiopharm. Synthesis of carbon-14 and stable isotope labeled Censavudine

[2] Junbiao Chang. Acc Chem Res. 4'-Modified Nucleosides for Antiviral Drug Discovery: Achievements and Perspectives

[3] Robert A Smith, et al. Antimicrob Agents Chemother. The Nucleoside Analog BMS-986001 Shows Greater In Vitro Activity against HIV-2 than against HIV-1

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Keywords: Censavudine, OBP-601; BMS-986001; TPN-101 supplier, HIV Protease, inhibitors, activators


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