RORγt Inverse agonist 10_product_DataBase

Bioactivity	RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R[1]
Invitro	RORγt Inverse agonist 10 has a good liver microsome stability (human CLint=0.010 mL/min/mg, mouse CLint=0.030 mL/min/mg)[1].RORγt Inverse agonist 10 suppresses the IL-17A production in a dose-dependent manner with an IC50 of 130 nM in a human whole-blood assay[1].
In Vivo	RORγt Inverse agonist 10 (3-100 mg/kg; p.o.) shows robust and dose-dependent inhibitory effect on the IL-17A production in mouse IL-18/23-induced cytokine expression model[1].RORγt Inverse agonist 10 (1.145 mg/kg; p.o.) shows a high AUC of 15000 nM*h and t1/2 of 3.6 hours[1]. Animal Model:
Name	RORγt Inverse agonist 10
CAS	2413986-35-1
Formula	C25H26F6N6O3
Molar Mass	572.50
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Reference	[1]. Ryota Nakajima, et al. Discovery of [1,2,4]Triazolo[1,5- a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists. ACS Med Chem Lett. 2020 Feb 27;11(4):528-534.

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