RORγt Inverse agonist 8_product_DataBase

Bioactivity	RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD[1].
Target	IC50: 19 nM (RORγt)
Invitro	RORγt Inverse agonist 8 (Cpd 1) is a potent RORγt inhibitor and binds to the ligand binding domain (LBD) of RORγt[1].RORγt Inverse agonist 8 (0-10μM ;24 hours) results in complete attenuation of IL-17A secretion in a concentration-dependent manner with an IC50 of 60 nM in HUT78 cells[1].RORγt Inverse agonist 8 selectively suppresses human Th17 and Tc17 cell differentiation[1].RORγt Inverse agonist 8 polarizes Th17 cells also blocks IL-17A production in a concentration-dependent manner with an IC50 of 92 nM[1].RORγt Inverse agonist 8 reduces Th17 cell-associated mRNA expression including IL17A, IL17F, IL26, IL23R and CCR6 in a concentration-dependent fashion[1].RORγt Inverse agonist 8 alters epigenetic regulation at the IL17A and IL23R gene promoters without impairing the DNA binding activity of RORγt[1].
In Vivo	RORγt Inverse agonist 8 (15 mg/kg, 45 mg/kg ; i.g.; twice daily; for 7 days) ameliorates antigen-induced arthritis (AiA) responses in Lewis rats[1]. Animal Model:
Name	RORγt Inverse agonist 8
CAS	2079892-79-6
Formula	C26H33N7O2
Molar Mass	475.59
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Guendisch U, et al. Pharmacological inhibition of RORγt suppresses the Th17 pathway and alleviates arthritis in vivo. PLoS One. 2017 Nov 20;12(11):e0188391.

PeptideDB

RORγt Inverse agonist 8

CAS: 2079892-79-6 F: C26H33N7O2 W: 475.59