GPR183 antagonist 33

Chemical Structure : GPR183 antagonist 33

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货号: PC-21880Not For Human Use, Lab Use Only.

GPR183 antagonist 33 is a highly potent, selective GPR183 (Epstein–Barr-virus-induced gene 2, EBI2) antagonist with IC50 of 0.83 nM in cAMP assays, and 1.83 nM in CER-reporter assays.

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生物&药学活性

GPR183 antagonist 33 is a highly potent, selective GPR183 (Epstein–Barr-virus-induced gene 2, EBI2) antagonist with IC50 of 0.83 nM in cAMP assays, and 1.83 nM in CER-reporter assays.
GPR183 antagonist 33 strongly reverses 7α,25-OHC-induced cAMP reduction in a dose-dependent manner with an IC50 value of 0.82 nM in HEK293-GPR183 cells.
GPR183 antagonist 33 shows minor impact on human GPCRome (168 nonolfactory GPCRs, including GPR183) using the PathHunter β-Arrestin assays.
GPR183 antagonist 33 exhibits strong suppressive activity against GPR183-mediated β-arrestin recruitment with an IC50 value of 0.88 nM.
GPR183 antagonist 33 displays strong in vitro antimigration and anti-inflammatory activity in monocytes, effectively blocks 7α,25-OHC induced cell migration in a dose-dependent manner with an IC50 value of 0.73 nM.
GPR183 antagonist 33 (3 mg/kg and 10 mg/kg, oral) effectively improves the pathological symptoms of DSS-induced experimental colitis.

物理化学性质&存储条件

分子量	471.37
分子式	C21H19BrN4O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(E)-1-(4-(2-Aminobenzo[d]thiazole-6-carbonyl)piperazin-1-yl)-3-(4-bromophenyl)prop-2-en-1-one

参考文献

1. Ruoqing Zeng, et al. J Med Chem. 2024 Feb 28. doi: 10.1021/acs.jmedchem.3c01905.