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 Details
| Formula: | C15H29N3O2 . HCl . H2O |
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| MW: | 283.3 . 36.5 . 18.0 |
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| Purity: | ≥98% (TLC) |
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| Appearance: | White solid. |
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| Solubility: | Soluble in water (5mg/ml), DMSO (2.5mg/ml) or 100% ethanol (5mg/ml). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Use/Stability: | Store solutions at -20°C for up to 3 months. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Protease activated‐receptor 2 is necessary for neutrophil chemorepulsion induced by trypsin, tryptase, or dipeptidyl peptidase IV: M.J.V. White, et al.; J. Leukoc. Biol.
103, 119 (2018),
Abstract;
Full Text
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;
