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Query String: VORAPAXAR

CHEMBL493982 Ethyl [(3aR,4aR,8aR,9aS)-9(S)-[(E)-2-[5-(3-fluorophenyl)-2-pyridinyl]ethenyl]dodecahydro-1(R)-methyl-3-oxonaphtho[2,3-c]furan-6(R)-yl]carbamate BDBM50261110 VORAPAXAR

Xia, Y; Chackalamannil, S; Greenlee, WJ; Wang, Y; Hu, Z; Root, Y; Wong, J; Kong, J; Ahn, HS; Boykow, G; Hsieh, Y; Kurowski, S; Chintala, M Discovery of a vorapaxar analog with increased aqueous solubility. Bioorg Med Chem Lett 20: 6676-9 (2010)
Fan, M; Han, M; Xia, Y; Zhang, Y; Chu, Y; Bai, G; Li, W; Li, J; Zhao, L; He, Y; Ma, X; Duan, Z Design and synthesis of potent PAR-1 antagonists based on vorapaxar. Bioorg Med Chem Lett 30: (2020)
Chelliah, MV; Eagen, K; Guo, Z; Chackalamannil, S; Xia, Y; Tsai, H; Greenlee, WJ; Ahn, HS; Kurowski, S; Boykow, G; Hsieh, Y; Chintala, M Himbacine-derived thrombin receptor antagonists: c7-spirocyclic analogues of vorapaxar. ACS Med Chem Lett 5: 561-5 (2014)
Chelliah, MV; Chackalamannil, S; Xia, Y; Greenlee, WJ; Ahn, HS; Kurowski, S; Boykow, G; Hsieh, Y; Chintala, M Himbacine-derived thrombin receptor antagonists: c7-aminomethyl and c9a-hydroxy analogues of vorapaxar. ACS Med Chem Lett 5: 183-7 (2014)

Trypin Activated FLPR Assay Calcium mobilization was measured using 1321N1 cells stably expressing human PAR2. Cells were seeded in 384-well plates at 4,000 cells per well in 20 μl DMEM with Glutamax supplemented with 10% FBS and incubated for 18-24 h at 37� C., 5% CO2 and 95% humidity. Cells were loaded with 20 μl Fluo-8 NW calcium dye (Cat: 36316, AAT Bioquest) and kept at 37� C. for 30 min prior to addition of 10 μl compound prepared in 20 mM HEPES pH 7.4, HBSS, 2.5% DMSO, 0.1% BSA and 6 μM Vorapaxar (to block Trypsin induced activity of PAR1). The addition was done using a FLIPRTETRA (384-well head, Molecular Devices) and the response was read simultaneously to detect any agonist activity. The cells were incubated for 30 min at room temperature with the compounds and were then evaluated for antagonist activity by addition of 10 μl 234 nM Trypsin prepared in 20 mM HEPES pH 7.4, HBSS and 0.1% BSA and simultaneous detection of calcium mobilization using the FLIPRTETRA.