RWJ 56110

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Cat.No. 2614 - RWJ 56110 | C41H43Cl2F2N7O3.2HCl | CAS No. 252889-88-6
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)
Datasheet
Citations (3)
Literature

Biological Activity

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

M. Wt 863.65
Formula C41H43Cl2F2N7O3.2HCl
Storage Store at -20°C
Purity ≥96% (HPLC)
CAS Number 252889-88-6
PubChem ID 90488773
InChI Key MGZSVSHDIOPSBO-ZEUUMAKDSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

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

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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

3 Citations for RWJ 56110

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

Juncker-Jensen et al (2013) Tumor MMP-1 activates endothelial PAR1 to facilitate vascular intravasation and metastatic dissemination. Cancer Res 73 4196 PMID: 23687338

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

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


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