Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R.
Description | RORγt Inverse agonist 10 is a highly potent and orally bioavailable compound that acts as an antagonist for the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt). With an IC50 of 51 nM, it effectively inhibits the activity of RORγt, a prominent transcription factor involved in the regulation of genes associated with the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R. |
Targets&IC50 | RORγt:51 nM (IC50) |
In vitro | RORγt Inverse Agonist 10 exhibits robust stability in liver microsomes, as demonstrated by its clearance rates (human CLint = 0.010 mL/min/mg, mouse CLint = 0.030 mL/min/mg)[1]. Additionally, it effectively inhibits IL-17A production in a dose-dependent manner, achieving an IC50 of 130 nM in human whole-blood assays[1]. |
In vivo | RORγt Inverse Agonist 10, administered orally at doses ranging from 3 to 100 mg/kg, significantly suppresses IL-17A production in a dose-dependent manner within a C57/BL6 male mice model employing IL-18/23-induced cytokine expression[1]. Furthermore, an oral dose of 1.145 mg/kg of the same compound has demonstrated a considerable pharmacokinetic profile with an area under the curve (AUC) of 15000 nM*h and a half-life (t 1/2) of 3.6 hours[1]. This study underscores the compound's potential in modulating immune responses through the targeted inhibition of IL-17A production. |
Molecular Weight | 572.512 |
Formula | C25H26F6N6O3 |
CAS No. | 2413986-35-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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RORγt Inverse agonist 10 2413986-35-1 RORrt Inverse agonist 10 RORgammat Inverse agonist 10 inhibitor inhibit