RORγt Inverse Agonist II, GSK805,10MG,5313690001,Sigma

销售价: ¥ 2548.92 / 件
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订货号 0BV3469
品牌型号 Sigma 5313690001
货期 询货期
最小订货量 1件
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产品介绍 Product Description

General description

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.


Biochem/physiol Actions

Cell permeable: yes
Primary Target
RORγt
Reversible: yes


Packaging

Packaged under inert gas


Preparation Note

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


Other Notes

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


Legal Information

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


Disclaimer

Toxicity: Standard Handling (A)


技术参数 Specifications
assay≥95% (HPLC)
Quality Level100
formpowder
manufacturer/tradenameCalbiochem®
storage conditionOK to freeze,protect from light
color off-white
solubilityDMSO: 100 mg/mL
storage temp.2-8°C
SMILES stringFC(F)(F)Oc1c(cccc1)c2c(cc(cc2Cl)NC(=O)Cc3ccc(cc3)[S](=O)(=O)CC)Cl
InChI keyCEICQMBWAQAIQX-UHFFFAOYSA-N
长度(mm)
宽度(mm)
高度(mm)
重量(kg)
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