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ENMD-1068

Proteinase-activated receptor ligand
 
BML-N110-0005 5 mg 97.00 USD
 
BML-N110-0025 25 mg 384.00 USD
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Selective PAR-2 antagonist. Dose dependently inhibits calcium signaling in Lewis lung carcinoma cells stimulated with a soluble peptide PAR-2 agonist or trypsin, but not with a soluble PAR-1 agonist. Does not inhibit platelet aggregation stimulated by thrombin suggesting that it does not inhibit PAR-3 or PAR-4 signaling. Reduces TNF-α and IL-1β production from rheumatoid arthritis synovial primary cell culture and reduces joint swelling in a carageenan/kaolin-injected mouse model.

Product Specification

Formula:C15H29N3O2 . HCl . H2O
 
MW:283.3 . 36.5 . 18.0
 
Purity:≥98% (TLC)
 
Appearance:White solid.
 
Solubility:Soluble in water (5mg/ml), DMSO (2.5mg/ml) or 100% ethanol (5mg/ml).
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Store solutions at -20°C for up to 3 months.
 
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Product Literature References

Protease-activated receptor 1 and 2 contribute to angiotensin II-induced activation of adventitial fibroblasts from rat aorta: R.Q. He, et al.; Biochem. Biophys. Res. Commun. 473, 517 (2016), Application(s): Cell culture, Abstract;
Trypsin, Tryptase, and Thrombin Polarize Macrophages towards a Pro-Fibrotic M2a Phenotype: M.J. White, et al. ; PLoS One 10, e0138748 (2015), Application(s): Cell Culture, Abstract; Full Text
Targeting proteinase-activated receptors: therapeutic potential and challenges: R. Ramachandran, et al.; Nat. Rev. Drug Discov. 11, 69 (2012), Abstract;
Expression and proinflammatory role of proteinase-activated receptor 2 in rheumatoid synovium: ex vivo studies using a novel proteinase-activated receptor 2 antagonist: E.B. Kelso, et al.; Arthritis Rheum. 56, 765 (2007), Abstract;
Therapeutic promise of proteinase-activated receptor-2 antagonism in joint inflammation: E.B. Kelso, et al.; J. Pharmacol. Exp. Ther. 316, 1017 (2006), Abstract;

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