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RORγt inhibitor 1

Chemical Structure RORγt inhibitor 1

CAS No.: 2079892-79-6

RORγt inhibitor 1

Catalog No.GY05769Research Only, Not for Human Use!

RORγt inhibitor 1 is a potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays

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Purity & Documentation Purity: > 98%(HPLC) Select Batch:

Biological Activity

RORγt inhibitor 1 is a potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays; shows no inhibitory activity against the closely related nuclear hormone receptors RORα or RORβ; attenuates expression of genes such as IL26, IL23R and CCR6 in primary human Th17 cells, attenuate the knee swelling response in an antigen-induced arthritis rat models and inhibits IL-17A cytokine production in ex vivo recall assays.

Physicochemical Properties

M.Wt 475.597
Formula C26H33N7O2
CAS No. 2079892-79-6
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
Shipping
Solubility

Chemical Name (S)-N-(8-((4-(cyclopentanecarbonyl)-3-methylpiperazin-1-yl)methyl)-7-methylimidazo[1,2-a]pyridin-6-yl)-2-methylpyrimidine-5-carboxamide

Clinical Information


References

1. Guendisch U, et al. PLoS One. 2017 Nov 20;12(11):e0188391.

2. Hintermann S, et al. ChemMedChem. 2016 Dec 16;11(24):2640-2648.

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