Cis-Lomibuvir

Cis-Lomibuvir (cis-VX-222) is the cis-isomer of Lomibuvir. Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis[1]. cis-Lomibuvir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

[1026785-59-0]

Product Name Alternative

Cis-VX-222

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

DNA/RNA Synthesis; HCV

Type

Reference compound

Related Pathways

Anti-infection; Cell Cycle/DNA Damage

Applications

COVID-19-anti-virus

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/cis-lomibuvir.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=C(N([C@H]2CC[C@@H](O)CC2)C([C@H]3CC[C@H](C)CC3)=O)C=C(C#CC(C)(C)C)S1)O

Molecular Formula

C25H35NO4S

Molecular Weight

445.61

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P362+P364-P405-P501

References & Citations

[1]Yi G, Deval J, et al. Biochemical study of the comparative inhibition of hepatitis C virus RNA polymerase by VX-222 and filibuvir. Antimicrob Agents Chemother. 2012;56 (2) :830-837.|[2]Li P, Dorsch W, et al. Discovery of Novel Allosteric HCV NS5B Inhibitors. 2. Lactam-Containing Thiophene Carboxylates. ACS Med Chem Lett. 2017;8 (2) :251-255. Published 2017 Jan 31.