Boceprevir, Antiviral; SARS-CoV-2 Mpro inhibitor (TBI5087)

Description

Product Details

Formal Name: (1R,2S,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-3-azabicyclo[3.1.0]hexane-2-carboxamide

Alternate Names: SCH 503034

Molecular Formula: C₂₇H₄₅N₅O₅

Formula Weight: 519.7

CAS Number: 394730-60-0

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 15 mg/ml); or Ethanol (25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Antiviral; SARS-CoV-2 Mpro inhibitor

Functions

Boceprevir directly inhibits Hepatitis C virus (HCV) NS3 protease (overall binding constant for formation of covalent adduct, Ki* = 14 nM; initial inhibition constant Ki = 7.8 µM). This blocks NS3 autoactivation, and subsequent cleavage and maturation of other viral proteins necessary for replisome assembly. This reversible, slow-binding ketoamide also restores host interferon signaling obstructed by HCV, thus reactivating the immune response. Recently, it was also found to inhibit the key SARS-CoV-2 protease, Mpro (3CLpro) in vitro (Ki = 1.18 µM) and in cells (EC50 = 1.9 µM, virus-induced cytopathic effects (CPE)

Application Procedures

First dissolved in DMSO (up to at least 15 mg/ml); or Ethanol (25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.