A GPR18 agonist
货号:ajcx23358
CAS:955121-65-0
分子式:C20H22N6O2
分子量：378.4
溶解度:DMF: 2 mg/ml,DMSO: 2 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PSB-KD107 is an agonist of the orphan G protein-coupled receptor GPR18 (EC₅₀= 0.56 µM in a β-arrestin recruitment assay using CHO cells expressing the human receptor).^1,2It is selective for GPR18 over GPR55, as well as cannabinoid (CB) receptor 1 (CB₁) and CB₂, at 10 µM but also binds to the adenosine A_2Areceptor (K_i= 0.33 µM for the rat receptor).^1,3

1.Schoeder, C.T., Kaleta, M., Mahardhika, A.B., et al.Structure-activity relationships of imidazothiazinones and analogs as antagonists of the cannabinoid-activated orphan G protein-coupled receptor GPR18Eur. J. Med. Chem.155381-397(2018) 2.Schoeder, C.T., Mahardhika, A.B., Drabczyńska, A., et al.Discovery of tricyclic xanthines as agonists of the cannabinoid-activated orphan G?protein-coupled receptor GPR18ACS Med. Chem. Lett.(2020) 3.Drabczyńska, A., MÜller, C.E., Schiedel, A., et al.Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: Structure-activity relationships as adenosine A1 and A2A receptor ligandsBioorg. Med. Chem.15(22)6956-6974(2007)