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Elbasvir

Cat. No. M2203
Elbasvir Structure
Synonym:

MK-8742

Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 150  USD150 In stock
50mg USD 440  USD440 In stock
100mg USD 650  USD650 In stock
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Quality Control & Documentation
Biological Activity

Elbasvir (MK-8742) is an inhibitor of Hepatitis C Virus (HCV) non-structural protein 5A (NS5A) that is being developed for the treatment of HCV infection. Elbasvir has broad, potent HCV genotypic activity in vitro against viral variants that are resistant to other NS5A inhibitors. Elbasvir (MK-8742) exhibits potent antiviral activity during 5 days of monotherapy in patients with GT1 and GT3 chronic HCV infection.

Chemical Information
Molecular Weight 882.02
Formula C49H55N9O7
CAS Number 1370468-36-2 (1444832-51-2)
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] Lahser FC, et al. Antimicrob Agents Chemother. The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons.

[2] Liu R, et al. Antimicrob Agents Chemother. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor elbasvir.

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Keywords: Elbasvir, MK-8742 supplier, HCV Protease, inhibitors, activators


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