RWJ-56110

• Description :

  RWJ-56110 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 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 inhibits angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 induces cell apoptosis[1][2].

• CAS Number :

  [252889-88-6]

• 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.html

• Solubility :

  10 mM in DMSO

• 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

• Molecular Formula :

  C41H43Cl2F2N7O3

• Molecular Weight :

  790.73

• 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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  PAR1