RORγt inhibitor 1|CAS 2079892-79-6

Cas No.:	2079892-79-6
Chemical Name:	(S)-N-(8-((4-(cyclopentanecarbonyl)-3-methylpiperazin-1-yl)methyl)-7-methylimidazo[1,2-a]pyridin-6-yl)-2-methylpyrimidine-5-carboxamide
SMILES:	C(C)1=NC=C(C(NC2=CN3C=CN=C3C(CN3CCN(C(C4CCCC4)=O)[C@H](C)C3)=C2C)=O)C=N1
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO

Description:

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 CC

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC73863	ODH-08	ODH-08 is a novel specific small molecule ligand and agonist of RORα with KD value of 8.4 um, shows potent antifibrotic effect. ODH-08 does not activate other nuclear receptors involved in lipid metabolism such as PPARα, PPARγ, PPARδ, and LXRα. ODH-08 reduces hepatic collagen deposition and expression levels of fibrogenic markers such as α-smooth muscle actin and collagen type I alpha 1 chain in Western diet-fed mice. ODH-08 suppresses the expression of fibrogenic proteins in hepatic stellate cells (HSCs). ODH-08 suppresses the activity of SMAD2 and 3, which are the primary downstream proteins of transforming growth factor β.
DC70267	BMS-986313	BMS-986313 is a potent, selective, orally active RORγt inverse agonist with EC50 of 3.6 nM in GAL-4 reporter assay in Jurkat cell line, and 50 nM in IL-17 human whole blood assay.BMS-986313 demonstrated robust efficacy in preclinical models of psoriasis (the IMQ-induced skin lesion model and the IL-23-induced acanthosis model).
DC47003	Bevurogant	Bevurogant is a retinoid-related orphan receptor-gamma t (RORγt) antagonist. Bevurogant can be used for the research of chronic inflammatory diseases.
DC46880	Cedirogant	Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.
DC44172	RORγt inverse agonist 13	RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved drug-like properties, with an IC50 of 63.8 nM.
DC44171	RORγt Inverse agonist 6	RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.
DC40965	BMS-986251	BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced models (preclinical models of psoriasis).
DC28745	FM26	FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells.
DC11869	RORγt inhibitor 1	A potent, selective, orally bioavailable RORγt inverse agonist with IC50 of 17 nM in TR-FRET assays
DC11846	TMP778	TMP778 (TMP-778) is a potent, selective RORγt inhibitor with IC50 of 7 nM in FRET assays and 63 nM in IL-17 promoter assays, with no inverse agonist activity.