315203-31-7
Chemical Structure
RWJ-58259
- CAS No.: 315203-31-7
- Formula:C40H42Cl2F2N8O3
- Molecular Weight:791.72
InChIKey: KEDDGIDZMJSBEW-PXLJZGITSA-N
SMILES: FC(C=C1C[C@@H](C(N[C@@H](CCN)C(NCC2=CC=CC=C2)=O)=O)NC(NC3=CC=C(C(CN4CCCC4)=N5)C(N5CC6=C(C=CC=C6Cl)Cl)=C3)=O)=C(C=C1)F
Biological Activity: RWJ-58259 is a selective PAR-1 inhibitor with an IC50 value of 0.15 μM. RWJ-58259 binds selectively to PAR-1, blocks the binding of tethered ligands, interferes with calcium mobilization and PAR-1-related cellular functions, and exhibits no PAR-1 agonist activity or thrombin proteolytic inhibitory activity. RWJ-58259 inhibits thrombin-induced platelet aggregation, calcium signaling and vascular smooth muscle cell proliferation, reduces neointimal thickness and arterial stenosis, and alleviates vascular occlusion and platelet deposition. RWJ-58259 can be used in the research of thrombotic diseases and vascular injury associated with acute coronary intervention[1][2].
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RWJ-58259 | RWJ-58259 is a selective PAR-1 inhibitor with an IC50 value of 0.15 μM. RWJ-58259 binds selectively to PAR-1, blocks the binding of tethered ligands, interferes with calcium mobilization and PAR-1-related cellular functions, and exhibits no PAR-1 agonist activity or thrombin proteolytic inhibitory activity. RWJ-58259 inhibits thrombin-induced platelet aggregation, calcium signaling and vascular smooth muscle cell proliferation, reduces neointimal thickness and arterial stenosis, and alleviates vascular occlusion and platelet deposition. RWJ-58259 can be used in the research of thrombotic diseases and vascular injury associated with acute coronary intervention. | |||||||||||||||||||||
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References
- [1]. Maryanoff BE, et al. Discovery of potent peptide-mimetic antagonists for the human thrombin receptor, protease-activated receptor-1 (PAR-1). Curr Med Chem Cardiovasc Hematol Agents. 2003;1(1):13-36. [Content Brief]
- [2]. Damiano BP, et al. RWJ-58259: a selective antagonist of protease activated receptor-1. Cardiovasc Drug Rev. 2003;21(4):313-326. [Content Brief]
