Timapiprant-OC000459-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETimapiprantCat. No.: HY-15342CAS No.: 851723-84-7Synonyms: OC000459分式: CHFNO分量: 348.37作靶点: Prostaglandin Receptor作通路: GPCR/G Protein储存式: 4C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitrogen

2、)溶解性数据体外实验 DMSO : 4 mg/mL (11.48 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 0.4 mg/mL (1.15 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 Timapiprant (OC000459)种效选择性的服型 D 前列腺素受体 2 (DP2，也称为 CRTH2) 拮抗剂。Timapiprant (OC000459) 有效地置

3、换来重 组 DP2 (K i=13 nM)，重 组DP2 ( K i=3 nM) 和天然 DP2 ( Ki=4 nM) 的 3H PGD2。 Timapiprant (OC000459) 抑制肥细胞激活 Th2 淋巴细胞和嗜酸性粒细胞。IC50 & Target Ki: 0.013 M (human recombinant DP2); 0.003 M (rat recombinant DP2) and 0.004 M (human native DP2)1体外研究 Timapiprant (OC000459) (0.0001 M-10 M; 5 hours) inhibits chemotax

4、is (IC50=0.028 M) of human Th2lymphocytes and cytokine production (IC50=0.019 M) by human Th2 lymphocytes 1.Timapiprant(OC000459) (1 M) inhibits the activation of Th2 cells and eosinophils in response to supernatants fromIgE/anti-IgE-activated human mast cells 1.Timapiprant (OC000459) (1 nM1000 nM;

5、16 hours) inhibits theanti-apoptotic effect of PGD2 on Th2 cells with an IC50 of 0.035 uM 1.Apoptosis Analysis 1Cell Line: Th2 CellsConcentration: 0.0001 M-10 MIncubation Time: 16 hoursResult: Inhibited the antiapoptotic effect of PGD2.体内研究 Timapiprant (OC000459) (gavage; 2 mg/kg, 10 mg/kg) inhibits

6、 blood eosinophilia induced by 13,14-dihydro-15-keto-PGD2 (DK-PGD2) in Rat (ED50=0.04 mg/kg) 1. Timapiprant (OC000459) (gavage; 0.01 mg/kg, 0.1mg/kg, 1.0 mg/kg) inhibits airway eosinophilia in response to an aerosol of DK-PGD2 in guinea pigs(ED50=0.01 mg/kg) 1.户使本产品发表的科研献 Allergol Int. 2016 Oct;65(4

7、):414-419.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Pettipher R, Vinall SL, Xue L, Pharmacologic profile of OC000459, a potent, selective, and orally active D prostanoid receptor 2antagonist that inhibits mast cell-dependent activation of T helper 2 lymphocytes and eosinophils. J Pharmacol Exp Ther. 2012Feb;340(2):473-82.McePdfHeightCaution: Product has not been fully validated for medical applications.For researc