Bioactivity | 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[1]. | |||||||||
Invitro | RORγt inverse agonist 13 (Compound 3i) exhibits activity with an inhibition of 76% at 0.3 µM in Th17 cell differentiation assay[1]. | |||||||||
In Vivo | RORγt inverse agonist 13 (Compound 3i, 25 mg/kg, Orally, twice daily) demonstrats excellent in vivo PK profile in mice and good in vivo efficacy in an IMQ-induced psoriasis mice model[1]. Animal Model: | |||||||||
Name | RORγt inverse agonist 13 | |||||||||
CAS | 2170477-75-3 | |||||||||
Formula | C23H17Cl2F3N2O4 | |||||||||
Molar Mass | 513.29 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [1]. Nannan Sun, et al. Discovery of carboxyl-containing biaryl ureas as potent RORγt inverse agonists. Eur J Med Chem. 2020 Jul 5;202:112536. |