RWJ-56110 (dihydrochloride)

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566) . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis[1][2].

Product Specifications

CAS Number

[2387505-58-8]

UNSPSC

12352005

Target

Apoptosis; Protease Activated Receptor (PAR)

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein

Applications

Neuroscience-Neurodegeneration

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/rwj-56110-dihydrochloride.html

Purity

99.87

Solubility

DMSO : 200 mg/mL (ultrasonic)

Smiles

O=C(N[C@H](C(NCC1=CC=CC=C1)=O)CCN)[C@@H](NC(NC2=CC3=C(C=C2)C(CN4CCCC4)=CN3CC5=C(Cl)C=CC=C5Cl)=O)CC6=CC=C(F)C(F)=C6.[H]Cl.[H]Cl

Molecular Formula

C41H45Cl4F2N7O3

Molecular Weight

863.65

References & Citations

[1]Andrade-Gordon, et al.Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. oc Natl Acad Sci U S A. 1999 Oct 26;96 (22) :12257-62.|[2]Panagiota Zania, et al. Blockade of angiogenesis by small molecule antagonists to protease-activated receptor-1: association with endothelial cell growth suppression and induction of apoptosis. J Pharmacol Exp Ther. 2006 Jul;318 (1) :246-54.