切换导航

AC 264613

Catalog No.
A8670
PAR2激动剂
组合的产品项目
规格价格库存 数量
10mg
¥ 3,760.00
Ship with 10-15 days
50mg
¥ 16,280.00
Ship with 10-15 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

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

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt400.27
Cas No.1051487-82-1
FormulaC19H18BrN3O2
Solubility<40.03mg/ml in DMSO
Chemical Name(3S,4R)-N-[(Z)-1-(3-bromophenyl)ethylideneamino]-2-oxo-4-phenylpyrrolidine-3-carboxamide
SDFDownload SDF
Canonical SMILESCC(=NNC(=O)C1C(CNC1=O)C2=CC=CC=C2)C3=CC(=CC=C3)Br
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

AC 264613