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Narlaprevir

Cat. No. M30743
Narlaprevir Structure
Synonym:

SCH 900518

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Quality Control & Documentation
Biological Activity

Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM. Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease. Narlaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.3 μM.

Chemical Information
Molecular Weight 707.96
Formula C36H61N5O7S
CAS Number 865466-24-6
Form Solid
Solubility (25°C) DMSO ≥ 50 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] I P Grushko, et al. Ter Arkh. [Comparative evaluation of the effectiveness of narlaprevir in the composition of interferon and interferon-free treatment regimens for patients with chronic hepatitis C]

[2] Daniel W Kneller, et al. Nat Commun. Covalent narlaprevir- and boceprevir-derived hybrid inhibitors of SARS-CoV-2 main protease

[3] Daniel Kneller, et al. Res Sq. Covalent narlaprevir- and boceprevir-derived hybrid inhibitors of SARS-CoV-2 main protease: room-temperature X-ray and neutron crystallography, binding thermodynamics, and antiviral activity

[4] Ashok Arasappan, et al. ACS Med Chem Lett. Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor

[5] Joep de Bruijne, et al. Hepatology. Antiviral activity of narlaprevir combined with ritonavir and pegylated interferon in chronic hepatitis C patients

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Keywords: Narlaprevir, SCH 900518 supplier, Anti-infection, inhibitors, activators


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