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GB-110 hydrochloride
本半岛bd体育手机客户端 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。
GB-110 hydrochloride图片
包装与价格:
包装 价格(元)
10mM (in 1mL DMSO) 电议
5mg 电议
10mg 电议
25mg 电议
50mg 电议
100mg 电议
200mg 电议
500mg 电议

半岛bd体育手机客户端 介绍
GB-110 hydrochloride 是一种有效的,具有口服活性的,非肽类的 protease activated receptor 2 (PAR2) 激动剂。GB-110 hydrochloride 选择性诱导 PAR2 介导的 HT29 细胞内 Ca2+ 释放,EC50 值为 0.28 μM。
Canonical SMILES O=C(C1=CC=NO1)N[C@@H](CC2CCCCC2)C(N[C@@H]([C@@H](C)CC)C(NCC3=CC=CC(C(N4CCC(CN)CC4)=O)=C3)=O)=O.Cl
分子式 C33H49ClN6O5
分子量 645.23
溶解度 DMSO: 125 mg/mL (193.73 mM)
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist. GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM[1].

In an intracellular Ca2+ (iCa2+) mobilization assay using HT29 colon cancer cells, GB110 (EC50 240±20 nM; pEC50 6.7±0.05) is equipotent with the peptide agonist 2f-LIGRLO-NH2 (EC50 210±30 nM; pEC50 6.6±0.05), 10-fold more potent than SLIGRL-NH2, but ~35-fold less potent than trypsin (EC50 6±0.5 nM; pEC50 8.2±0.8)[2].

[1]. Barry GD, et al. Novel agonists and antagonists for human protease activated receptor 2. J Med Chem. 2010 Oct 28;53(20):7428-40. [2]. Suen JY, et al. Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110). Br J Pharmacol. 2012 Mar;165(5):1413-23.

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