RWJ 56110

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Description: Selective PAR1 antagonist
Chemical Name: (αS)-N-[(1S)-3-Amino-1-[[(phenylmethyl)amino]carbonyl]propyl]-α-[[[[1-[(2,6-dichlorophenyl)methyl]-3-(1-pyrrolidinylmethyl)-1H-indol-6-yl]amino]carbonyl]amino]-3,4-difluoro-benzenepropanamide
Purity: ≥96% (HPLC)
Citations (5)

Biological Activity for RWJ 56110

RWJ 56110 is a selective protease-activated receptor-1 (PAR1) antagonist; displays no activity at PAR2, PAR3, or PAR4 subtypes. Blocks thrombin-induced platelet aggregation and activation of MAPK in HUVECs. Also inhibits angiogenesis in a chick embryo angiogenesis model in vivo.

Technical Data for RWJ 56110

M. Wt 863.65
Formula C41H43Cl2F2N7O3.2HCl
Storage Store at -20°C
Purity ≥96% (HPLC)
CAS Number 2387505-58-8
PubChem ID 90488773
Smiles ClC1=CC=CC(Cl)=C1CN3C2=CC(NC(N[C@@H](CC5=CC(F)=C(F)C=C5)C(N[C@@H](CCN)C(NCC6=CC=CC=C6)=O)=O)=O)=CC=C2C(CN4CCCC4)=C3.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for RWJ 56110

Solvent Max Conc. mg/mL Max Conc. mM
water 21.59 25
DMSO 86.36 100

Preparing Stock Solutions for RWJ 56110

The following data is based on the product molecular weight 863.65. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.16 mL 5.79 mL 11.58 mL
5 mM 0.23 mL 1.16 mL 2.32 mL
10 mM 0.12 mL 0.58 mL 1.16 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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Product Datasheets for RWJ 56110

Certificate of Analysis / Product Datasheet
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References for RWJ 56110

References are publications that support the biological activity of the product.

Maryanoff et al (2003) Discovery of potent peptide-mimetic antagonists for the human thrombin receptor, protease-activated receptor-1 (PAR-1). Curr.Med.Chem.Cardiovasc.Hematol.Agents 1 13 PMID: 15317288

Zania et al (2006) 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. 318 246 PMID: 16595737

Andrade-Gordon et al (1999) Design, synthesis and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. Proc.Natl.Acad.Sci.USA 96 12257 PMID: 10535908

If you know of a relevant reference for RWJ 56110, please let us know.

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Keywords: RWJ 56110, RWJ 56110 supplier, selective, PAR1, antagonists, PAR, receptors, protease-activated, proteinase-activated, RWJ56110, 252889-88-6, Protease-Activated, Receptors, 2614, Tocris Bioscience

5 Citations for RWJ 56110

Citations are publications that use Tocris products. Selected citations for RWJ 56110 include:

Eum et al (2014) Disruption of epithelial barrier by quorum-sensing N-3-(oxododecanoyl)-homoserine lactone is mediated by matrix metalloproteinases. Am J Physiol Gastrointest Liver Physiol 306 G992 PMID: 24742991

Xu et al (2015) Heat stress-induced disruption of endothelial barrier function is via PAR1 signaling and suppressed by Xuebijing injection. PLoS One 10 e0118057 PMID: 25693178

Shi et al (2019) Identification and therapeutic rescue of autophagosome and glutamate receptor defects in C9ORF72 and sporadic ALS neurons. JCI Insight 5 PMID: 31310593

Wang (2017) Complement-activation fragment C4a mediates effector functions by binding as untethered agonist to protease-activated receptors 1 and 4. Proc Natl Acad Sci U S A 114 10948 PMID: 28973891

Do you know of a great paper that uses RWJ 56110 from Tocris? Please let us know.

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