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AC 264613
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AC 264613图片
CAS NO:1051487-82-1
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
AC 264613 是一种有效的选择性蛋白酶激活受体 (PAR-2) 激动剂，pEC50 为 7.5。
Cas No.1051487-82-1
化学名(3S,4R)-N-[(Z)-1-(3-bromophenyl)ethylideneamino]-2-oxo-4-phenylpyrrolidine-3-carboxamide
Canonical SMILESCC(=NNC(=O)C1C(CNC1=O)C2=CC=CC=C2)C3=CC(=CC=C3)Br
分子式C19H18BrN3O2
分子量400.27
溶解度<40.03mg/ml in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.