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GNE-6468

Chemical Structure : GNE-6468

CAS No.: 1677668-27-7

GNE-6468 (GNE6468;GNE 6468)

Catalog No.: PC-35557Not For Human Use, Lab Use Only.

GNE-6468 (GNE6468) is a potent and selective RORc (RORγ) inverse agonist (EC50=2 nM) with >1,000-fold selectivity for RORc over PPARγ.

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Biological Activity

GNE-6468 (GNE6468) is a potent and selective RORc (RORγ) inverse agonist (EC50=2 nM) with >1,000-fold selectivity for RORc over PPARγ.
GNE-6468 displays excellent selectivity profiles against a panel of other nuclear receptors in Gal4 human transcription assays.
GNE-6468 displays potent inhibition of IL-17 production with EC50 of 30 nM in human PBMC cytokine production assays, without effect on IFNγ production.
GNE-6468 is a chemical biology tool to further explore the role of RORc in human biology.

Physicochemical Properties

M.Wt 433.85
Formula C23H16ClN3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(6-(2-chloro-6-cyclopropylbenzoyl)imidazo[1,5-a]pyrimidin-8-yl)-2-hydroxybenzoic acid

References

1. Fauber BP, et al. Bioorg Med Chem Lett. 2015 Aug 1;25(15):2907-12.

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