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Chemical Structure : GPR183 antagonist 33
Catalog No.: 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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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.
| M.Wt | 471.37 | |
| Formula | C21H19BrN4O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ruoqing Zeng, et al. J Med Chem. 2024 Feb 28. doi: 10.1021/acs.jmedchem.3c01905.
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