IC50: 28.5 nM (GPR183)[1]
SAE-14 (compound SAE-14) is a potent, specific GPR183 antagonist with an IC50 value of 28.5 nM, can antagonize 7α, 25-OHC-induced calcium mobilization with IC50 value below 50 nM in HL-60 cells. GPR183 antagonist-1 can reverse allodynia in mice[1].
SAE-14 (compound SAE-14) can able to antagonize 7α, 25-OHC-induced calcium mobilization with an IC50 value below 50 nM[1].
Cell Viability Assay[1]
| Cell Line: | The human leukemia (HL)-60 cells |
| Concentration: | 5×of the antagonist |
| Incubation Time: | 15 min |
| Result: | Had GPR183-specific (IC50: 28.5nM) and abolished 7a, 25-OHC-induced calcium mobilization in the HL-60 cells. |
SAE-14 (compound SAE-14) (i.th.; 2.9 µM; once) can reverse nerve injury-induced allodynia in mice[1].
| Animal Model: | Male and female ICR mice[1] |
| Dosage: | 2.9 µM |
| Administration: | intrathecal (i.th.) injections; 2.9 µM; once |
| Result: | Reversed CCI-induced mechanical allodynia in a time-dependent manner. |