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GSK805 is a potent, orally bioavailable RORγγ Inhibitor, with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay. GSK805 suppresses T helper 17 (Th17) responses, including IL-17 and IFN-γ production (~ 500 nM). GSK805 directly and reversibly interacts with the ligand binding domain of RORγt to block its transcriptional effects. GSK805 induces RORγt binding to Gata3 resulting in increased expression of GATA3. GSK805 reduces the severity of autoimmune encephalomyelitis in murine models of multiple sclerosis (30 mg/kg/day, p.o.).
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| Preparation method | |
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| Animal models | EAE mice |
| Formulation | |
| Dosages | once daily at 3 doses (1, 3, and 10 mg/kg) |
| Administration | orally |
| Molecular Weight | 532.36 |
| Formula | C23H18Cl2F3NO4S |
| CAS Number | 1426802-50-7 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ROR Products |
|---|
| Dehydrolithocholic acid
Dehydrolithocholic acid is a bile acid metabolite, which inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM). |
| SR3335
SR3335 (ML-176) is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays. |
| SR1078
SR1078 is an agonist of retinoic acid receptor-related orphan receptors (ROR) RORα/γ; increases transcription of RORα target genes; thought to increase p53 stability. |
| SR 1001
SR 1001 is a RORα/γ inverse agonist with Ki values of 172 and 111 nM, respectively. |
| GSK2981278
GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma). |
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