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Uprifosbuvir

Cat. No. M40994
Uprifosbuvir Structure
Synonym:

MK-3682; IDX21437

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Biological Activity

Uprifosbuvir is a nucleic acid NS5b polymerase inhibitor with antiviral activity and may be used in hepatitis C related studies.

Chemical Information
Molecular Weight 545.91
Formula C22H29ClN3O9P
CAS Number 1496551-77-9
Form Solid
Solubility (25°C) DMSO >100 mg/mL
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] Artis Klapars et al. Chem Sci. Efficient synthesis of antiviral agent uprifosbuvir enabled by new synthetic methods

[2] Paul van den Berg et al. CPT Pharmacometrics Syst Pharmacol. Understanding effect site pharmacology of uprifosbuvir, a hepatitis C virus nucleoside inhibitor: Case study of a multidisciplinary modeling approach in drug development

[3] Eric Lawitz et al. J Viral Hepat. Efficacy and safety of a two-drug direct-acting antiviral agent regimen ruzasvir 180 mg and uprifosbuvir 450 mg for 12 weeks in adults with chronic hepatitis C virus genotype 1, 2, 3, 4, 5 or 6

[4] Edward J Gane et al. Lancet Gastroenterol Hepatol. Safety and efficacy of an 8-week regimen of grazoprevir plus ruzasvir plus uprifosbuvir compared with grazoprevir plus elbasvir plus uprifosbuvir in participants without cirrhosis infected with hepatitis C virus genotypes 1, 2, or 3 (C-CREST-1 and C-CREST-2, part A): two randomised, phase 2, open-label trials

[5] David Wyles et al. Hepatology. Grazoprevir, ruzasvir, and uprifosbuvir for hepatitis C virus after NS5A treatment failure

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Keywords: Uprifosbuvir, MK-3682; IDX21437 supplier, Anti-infection, inhibitors, activators

 
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