Bioactivity | RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC50 of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis[1]. |
In Vivo | RORγt inverse agonist 14 (8e) exhibits t1/2 of 11 h by iv injection of 1 mg/kg. RORγt inverse agonist 14 (8e) exhibits tmax of 2 h, %F of 101 by oral administration of 4 mg/kg in mouse[1].RORγt inverse agonist 14 (8e, 5-20 mg/kg) provides essentially the same arthritic score reduction as a murine equivalent of the marketed TNF decoy receptor etanercept[1]. Animal Model: |
Name | RORγt inverse agonist 14 |
Formula | C26H26F8N2O6S2 |
Molar Mass | 678.61 |
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]. Qingjie Liu, et al. Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis. ACS Med Chem Lett. 2021 Apr 30;12(5):827-835. |