2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. 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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RWJ-58259

RWJ-58259 Chemical Structure

CAS No. : 315203-31-7

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RWJ-58259 Related Antibodies

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Description

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].

IC50 & Target[1]

PAR1

0.15 μM (IC50)

In Vitro

RWJ-58259 potently binds to PAR-1 in the cell membrane of CHRF-288-11, with an IC50 of 0.15 μM[1].
RWJ-58259 potently and selectively inhibits thrombin-induced aggregation (IC50 0.37 μM) and TRAP-6-induced aggregation (IC50 0.11 μM) of gel-filtered platelets, and shows no activity against collagen or U46619 at concentrations up to 50 μM[1].
RWJ-58259 potently inhibits α-thrombin-induced calcium mobilization in RASMC, with an IC50 of 0.07 μM[1].
RWJ-58259 inhibits α-thrombin-induced proliferation of RASMC with an IC50 of 2.3 μM[1].
RWJ-58259 potently inhibits α-thrombin-induced calcium mobilization in hPAR-1-transfected mouse pulmonary myofibroblasts with an IC50 of 0.31 μM; it also inhibits TRAP-6-induced calcium mobilization with an IC50 of 0.11 μM[1].
RWJ-58259 inhibits PAR-1-mediated calcium mobilization in hPAR-1-transfected cells, with an IC50 of 0.31 μM for thrombin-induced signaling pathways and an IC50 of 0.11 μM for SFLLRN-induced signaling pathways[2].
RWJ-58259 inhibits PAR-1-mediated proliferation in thrombin-induced rat vascular smooth muscle cells, with an IC50 of 2.3 μM[2].
RWJ-58259 inhibits thrombin-induced PAR-1-mediated IL-6 release in vascular smooth muscle cells, with an IC50 of 3.6 μM[2].
RWJ-58259 inhibits PAR-1-mediated microvascular growth in rat aortic ring models with an IC50 of 3 μM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RWJ-58259 Related Antibodies
In Vivo

RWJ-58259 (10 mg; periarterial administration; 14-day vascular injury restenosis experiment) significantly reduces neointimal formation, percentage of stenosis, neointimal thickness, and intima/media ratio in a rat carotid artery balloon angioplasty restenosis model[1].
Intravenous infusion of RWJ-58259 maintains plasma concentrations ≥12 μM, significantly prolongs occlusion time, completely prevents vascular occlusion in the tested arteries, reduces platelet-rich thrombus formation in a cynomolgus monkey arterial injury thrombosis model, and does not affect hemostatic parameters[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: unspecified strain[1]
Dosage: 10 mg
Administration: perivascular; 14-day vascular injury restenosis experiment
Result: Reduced intimal area to 0.084 mm2 compared to 0.129 mm2 in vehicle controls (p < 0.05).
Reduced percentage stenosis to 26% compared to 44% in vehicle controls (p < 0.05).
Reduced neointimal thickness to 45 μm compared to 77 μm in vehicle controls (p < 0.05).
Reduced intima/media ratio to 0.83 compared to 1.35 in vehicle controls (p < 0.05).
Animal Model: unspecified strain[1]
Dosage: A certain dose
Administration: i.v. infusion
Result: Attenuated or prevented vessel occlusion in 100% of treated vessels (N=9).
Achieved complete 60-minute patency in 5 out of 9 vessels.
Significantly increased time to occlusion compared to vehicle controls (p < 0.05).
Significantly reduced platelet deposition and shifted thrombi from platelet-rich to platelet-poor.
Caused no significant effects on key hematological or coagulation parameters.
Molecular Weight

791.72

Formula

C40H42Cl2F2N8O3
CAS No.
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
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RWJ-58259 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RWJ-58259315203-31-7RWJ58259RWJ 58259Protease Activated Receptor (PAR)Thrombin receptorsmouse lung myofibroblastsrestenosisthrombosisCHRF-288-11PAR-1human aortic smooth muscle cellsProtease-Activated Receptor-1RASMCrat aortic smooth muscle cellshuman plateletsInhibitorinhibitorinhibit

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RWJ-58259
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