RORγt inverse agonist 29_product_DataBase

Bioactivity	RORγt inverse agonist 29 is a potent, orally active and selective RORγt inverse agonist (IC50: 21 nM). RORγt inverse agonist 29 can be used in the research of skin inflammation and autoimmune diseases like psoriasis[1].
Invitro	RORγt inverse agonist 29 (compound b12) demonstrates high RORγt transcriptional inhibitory activity (IC50: 28 nM) in human Jurkat cells[1].RORγt inverse agonist 29 (10 μM) shows good metabolic stabilities in in vitro human liver microsomes, with comparable half-life (T1/2: 4.46 h) and HLM (CLint(liver): 4.8 mL/min/kg)[1].
In Vivo	RORγt inverse agonist 29 (p.o., 100 mg/kg) reduces the total Psoriasis Area and the development of clinical symptoms in mouse Imiquimod-induced skin inflammation model[1].RORγt inverse agonist 29 (i.v., p.o., 0.3 or 1 mg/kg) displays an acceptable bioavailability and a half-life in rats[1]. Animal Model:
Name	RORγt inverse agonist 29
Formula	C25H24N2O5S
Molar Mass	464.53
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]. Lei Chen, et al. Discovery of N-(2-benzyl-4-oxochroman-7-yl)-2-(5-(ethylsulfonyl) pyridin-2-yl) acetamide (b12) as a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist. Bioorg Chem. 2022 Feb;119

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