ENMD-1068

BML-N110

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Proteinase-activated receptor ligand

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.

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Product Details

Appearance	White solid.
Couple Target	Proteinase-activated receptor
Couple Type	Ligand
Formula	C₁₅H₂₉N₃O₂ . HCl . H₂O
MW	283.3 . 36.5 . 18.0
Purity	≥98% (TLC)
Solubility	Soluble in water (5mg/ml), DMSO (2.5mg/ml) or 100% ethanol (5mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Store solutions at -20°C for up to 3 months.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Platelet-activating factor and protease-activated receptor 2 cooperate to promote lung inflammation through nuclear factor-kappa B transactivation: Silva, I., Almeida, A., et al.; Authorea Preprints , (2023)
Platelet-activating factor and protease-activated receptor 2 cooperate to promote neutrophil recruitment and lung inflammation through nuclear factor-kappa B transactivation: Silva, I. S., Almeida, A. D., et al.; Sci. Rep. 13, 21637 (2023), Abstract
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
Transforming Growth Factor-β1/Activin Receptor-like Kinase 5-Mediated Cell Migration is Dependent on the Protein Proteinase-Activated Receptor 2 but not on Proteinase-Activated Receptor 2-Stimulated Gq-Calcium Signaling: Ungefroren, H., Witte, D., et al.; Mol. Pharmacol. 92, 519 (2017), Abstract
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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ENMD-1068

BML-N110

Product Details

Handling & Storage

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