Description
OC000459 is an indole-acetic acid derivative that potently displaces PGD2 from human recombinant D prostanoid receptor 2 with Ki of 13 nM, rat recombinant D prostanoid receptor 2 with Ki of 3 nM, and human native D prostanoid receptor 2 with Ki of 4 nM.
Alias
OC-000459, OC 000459
Storage
2 years -20centigrade Powder
Synonyms
OC-000459, OC 000459
Targets
human recombinant DP2
Molecular Formula
C21H17FN2O2
Chemical Name
5-fluoro-2-methyl-3-(2-quinolinylmethyl)-1H-indole-1-acetic acid
Solubility
DMSO:PBS(1:1) 0.5 mg/mL
In vitro
VX-950 is a potent, small molecule, peptidomimetic inhibitor of the hepatitis C virus (HCV) NS3.4A serine protease. Although competitive with the peptide substrate in the active site, VX-950 exhibits apparent noncompetitive inhibition as a result of its tight binding properties and time-dependent inhibition mechanism. Incubation of the HCV Con1 subgenomic replicon cells with VX-950 results in a concentration-dependent decline of the HCV RNA level. The dominant resistance mutation observed against VX-950 was a substitution of Ala156 in the HCV NS3 protease domain with a serine. VX-950 demonstrates excellent antiviral activity both in genotype 1b HCV replicon cells with IC50 of 354 nM and in human fetal hepatocytes infected with genotype 1a HCV-positive patient sera with IC50 of 280 nM. VX-950 forms a covalent but reversible complex with the genotype 1a HCV NS3-4A protease in a slow-on, slow-off process with a steady-state inhibition constant Ki of 7 nM. [1][2]
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