Sigma-Aldrich Rorgt Inverse Agonist Ii g

Assay

≥95% (HPLC)

Quality Level

100

Form

powder

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

off-white

Solubility

DMSO: 100 mg/mL

Storage Temp.

2-8°C

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 toGata3resulting 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 toGata3resulting 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: yesPrimary Target
RORγtReversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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