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AC 264613

Katalog-Nr.GC14831

AC 264613 ist ein potenter und selektiver Protease-aktivierter Rezeptor (PAR-2)-Agonist mit einem pEC50 von 7,5.

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AC 264613 Chemische Struktur

Cas No.: 1051487-82-1

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

AC 264613 is a potent agonist of PAR2 with pEC50 value of 7.5 and potencies range from 30 to 100 nM [1, 2].

Protease-activated receptor 2 (PAR2) also known as coagulation factor II (thrombin) receptor-like 1 (F2RL1) or G-protein coupled receptor 11 (GPR11) is expressed in vascular tissue and highly vascular organs and involves in the vascular tone regulation. It has been shown that PAR2 plays a pivotal role in vessel inflammation and wound healing processes [2].

AC 264613 is a selective PAR2 agonist and has no effect on other PARs. When tested with HEK 293 T cells (PAR2 wild type) and KNRK cells (transfected with human PAR2 receptors) for stimulates PI hydrolysis and Ca2+ mobilization assays, AC 264613 showed effect with pEC50 value of 6.9 and 7.0,respectively [1]. Using QuickChange Mutagenesis manner, NIH 3T3 cells were made with ECL2 mutations in Q233E, E232R, E232R/Q233R, F240S, and F240S/S37P receptors and AC 264613 treatment PAR2 F240S receptors were constitutively expressed in multiple functional endpoints while had no effect on E232 and Q233 mutaions [2].

In male Sprague-Dawley rat model with acute thermal nociception and edema in paw induced by SLIGRL-NH2 or trypsin, intrapaw administration of AC 264613 induced hind paw edema and thermal hyperalgesia at the doses as low as 30 ng and showed dose-dependent pronociceptive effects [1].

References:
[1].  Gardell, L.R., et al., Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther, 2008. 327(3): p. 799-808.
[2].   Ma, J.N. and E.S. Burstein, The protease activated receptor 2 (PAR2) polymorphic variant F240S constitutively activates PAR2 receptors and potentiates responses to small-molecule PAR2 agonists. J Pharmacol Exp Ther, 2013. 347(3): p. 697-704.

Chemical Properties

Cas No. 1051487-82-1 SDF
Chemical Name (3S,4R)-N-[(Z)-1-(3-bromophenyl)ethylideneamino]-2-oxo-4-phenylpyrrolidine-3-carboxamide
Canonical SMILES CC(=NNC(=O)C1C(CNC1=O)C2=CC=CC=C2)C3=CC(=CC=C3)Br
Formula C19H18BrN3O2 M.Wt 400.27
Löslichkeit <40.03mg/ml in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.4983 mL 12.4916 mL 24.9831 mL
5 mM 0.4997 mL 2.4983 mL 4.9966 mL
10 mM 0.2498 mL 1.2492 mL 2.4983 mL
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