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Chemical Structure : RWJ-58259
Catalog No.: PC-20577Not For Human Use, Lab Use Only.
RWJ-58259 (RWJ58259) is a potent, selective thrombin receptor PAR-1 antagonist with binding IC50 of 0.15 uM, and IC50 of 0.07 uM in RASMC calcium mobilization assays.
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RWJ-58259 (RWJ58259) is a potent, selective thrombin receptor PAR-1 antagonist with binding IC50 of 0.15 uM, and IC50 of 0.07 uM in RASMC calcium mobilization assays.
RWJ-58259 exhibit an IC50 of 0.02 uM in PAR1-mediated iCa2+ mobilization assay in presence of 5 μM TFLLRN-NH2.
RWJ-58259 demonstrated in vivo antirestenotic activity in a rat balloon angioplasty model.
Perivascular administration of RWJ-58259 (10 mg) significantly reduced neointimal thickness in rats.
| M.Wt | 791.73 | |
| Formula | C40H42Cl2F2N8O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Zhang HC, et al. J Med Chem. 2001 Mar 29;44(7):1021-4.
2. Andrade-Gordon P, et al. J Pharmacol Exp Ther. 2001 Jul;298(1):34-42.
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