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MK-5172 (Grazoprevir)

Cat. No. M3278
MK-5172 (Grazoprevir) Structure
Synonym:

Grazoprevir; MK5172

Size Price Availability Quantity
5mg USD 270  USD270 In stock
10mg USD 470  USD470 In stock
25mg USD 870  USD870 In stock
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Quality Control & Documentation
Biological Activity

MK-5172 is a novel NS3/4, a protease inhibitor for chronic HCV infection (Enzyme Ki for genotype1b, 2a, 2b and 3a at <0.02, 0.15, 0.02 and 0.7 nM, respectively). This agent has an attractive preclinical profile including high potency in vitro, significant liver exposure upon oral dosing, and potent inhibitory activity against viral variants that are resistant to other protease inhibitors in development. MK-5172 has also demonstrated anti-viral efficacy in a chimpanzee model of chronic HCV infection.

Chemical Information
Molecular Weight 766.9
Formula C38H50N6O9S
CAS Number 1350514-68-9
Solubility (25°C) DMSO 85 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] Vincenzo Summa, et al. Antimicrob Agents Chemother. MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants

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Keywords: MK-5172 (Grazoprevir), Grazoprevir; MK5172 supplier, HCV Protease, inhibitors, activators


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