Description
Timapiprant sodium (OC000459 sodium) is a potent, selective, and orally active D prostanoid receptor 2 ( DP 2, also known as CRTH2 ) antagonist. Timapiprant sodium (OC000459 sodium) potently displaces [ 3 H] PGD2 from human recombinant DP 2 ( K i =13 nM), rat recombinant DP 2 ( K i =3 nM), and human native DP 2 ( K i =4 nM). Timapiprant sodium (OC000459 sodium) inhibits mast cell activation of Th2 lymphocytes and eosinophilsIn VitroTimapiprant sodium (OC000459 sodium) (0.0001 µM-10 µM; 5 hours) inhibits chemotaxis (IC 50 =0.028 µM) of human Th2 lymphocytes and cytokine production (IC 50 =0.019 µM) by human Th2 lymphocytes. Timapiprant sodium (OC000459 sodium) (1 µM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells. Timapiprant sodium (OC000459 sodium) (1 nM-1000 nM; 16 hours) inhibits the anti-apoptotic effect of PGD2 on Th2 cells with an IC 50 of 0.035 uM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis AnalysisCell Line: Th2 Cells Concentration: 0.0001 µM-10 µM Incubation Time: 16 hours Result: Inhibited the antiapoptotic effect of PGD2.In VivoTimapiprant sodium (OC000459 sodium) (gavage; 2 mg/kg, 10 mg/kg) inhibits blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in Rat (ED 50 =0.04 mg/kg). Timapiprant sodium (OC000459 sodium) (gavage; 0.01 mg/kg, 0.1 mg/kg, 1.0 mg/kg) inhibits airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs (ED 50 =0.01 mg/kg). MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:Ki: 0.013 µM (human recombinant DP2),0.003 µM (rat recombinant DP2) and 0.004 µM (human native DP2)