GSK805

SKU: orb1220466

Description

GSK805 is a potent orally bioavailable retinoid-related orphan receptor gamma t (RORγt) inverse agonist that interacts with the receptor's putative ligand binding domain without exerting significant effects on DNA binding.

Key Properties

• CAS Number: 1426802-50-7
• MW: 532.36
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₈Cl₂F₃NO₄S
• SMILES: CCS(=O)(=O)c1ccc(CC(=O)Nc2cc(Cl)c(c(Cl)c2)-c2ccccc2OC(F)(F)F)cc1
• Target: ROR
• Solubility: DMSO:100 mg/mL (187.84 mM)

Bioactivity

• In Vivo:
  GSK805 (10 mg/kg; p.o. once per day for 35 days) improves the situation of mice with experimental autoimmune encephalomyelitis (EAE). GSK805 (30 mg/kg; p.o. once) inhibits Th17 cell responses in EAE mice. Animal model: C57BL/6 mice were immunized with MOG35–55 plus CFA. Dosage: 10 mg/kg. Administration: Oral gavage; 10 mg/kg once per day; for 35 days. Result: Efficiently ameliorated the severity of EAE in mice. Animal model: C57BL/6 mice with EAE. Dosage: 30 mg/kg. Administration: Oral gavage; 30 mg/kg once. Result: Reduced both IFN-γ-IL-17+ and IFN-γ+IL-17+ T cells without altered the frequency of TNF-α+ T cells in EAE mice.
• In Vitro:
  Cell Differentiation Assay Cell line: CD4+ T cells. Concentration: 0.5 μM Incubation time: 4 days. Result: Inhibited IL-17 production during Th17 cell differentiation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

ROR