5.31369

RORγt Inverse Agonist II, GSK805

• 别名: RORγt Inverse Agonist II, GSK805, N-(3,5-Dichloro-4-(2-(trifluoromethoxy)phenyl)phenyl)-2-(4-ethylsulfonylphenyl)acetamide, N-(2,6-Dichloro-2ʹ-(trifluoromethoxy)biphenyl-4-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide, Retinoid-related Orphan Receptor γ t Antagonist II, RORγt A
• 经验公式（希尔记法）: C₂₃H₁₈Cl₂F₃NO₄S
• CAS号: 1426802-50-7
• 分子量: 532.36
• MDL號碼: MFCD28902182
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 化驗: ≥95% (HPLC)
• 品質等級: 100
• 形狀: powder
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: FC(F)(F)Oc1c(cccc1)c2c(cc(cc2Cl)NC(=O)Cc3ccc(cc3)[S](=O)(=O)CC)Cl

说明

一般說明

A cell-permeable, orally available, non-toxic, conformationally restricted biaryl-amide compound that acts as a potent retinoid-related orphan receptor γt (RORγt) isoform selective inverse agonist and suppresses T helper 17 (Th17) responses, including IL-17 and IFN-γ production (~ 500 nM). Directly and reversibly interacts with the ligand binding domain of RORγt to block its transcriptional effects, however, it does not affect RORγt binding to DNA. Induces RORγt binding to Gata3 resulting in increased expression of GATA3. Reduces the severity of autoimmune encephalomyelitis in murine models of multiple sclerosis (30 mg/kg/day, p.o.).

A cell-permeable, orally available, non-toxic, conformationally restricted biaryl-amide compound that acts as a potent retinoid-related orphan receptor γt (RORγt) isoform selective inverse agonist and suppresses T helper 17 (Th17) responses, including IL-17 and IFN-γ production (~ 500 nM). Directly and reversibly interacts with the ligand binding domain of RORγt to block its transcriptional effects, however, it does not affect RORγt binding to DNA. Induces RORγt binding to Gata3 resulting in increased expression of GATA3. Reduces the severity of autoimmune encephalomyelitis in murine models of multiple sclerosis (30 mg/kg/day, p.o.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化／生理作用

Cell permeable: yes

Primary Target
RORγt

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Xiao, S., et al. 2014. Immunity.40, 477.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable