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。
货号:ajcx14624
CAS:N/A
分子式:C33H49ClN6O5
分子量：645.23
溶解度:DMSO: 125 mg/mL (193.73 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.