Bioactivity | RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo[1]. | ||||||||||||
In Vivo | RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in a mouse pharmacodynamics model[1].RORγt Inverse agonist 6 (compound 43) exhibits improved drug exposure (mouse AUC: 1289 ng•h/mL at 1 mg/kg, po)[1].RORγt Inverse agonist 6 (compound 43, 30 mg/kg, po, b.i.d) inhibits the expression level of IL-17A by 59% compared to the vehicle after the oral administration at the tested dose[1]. Animal Model: | ||||||||||||
Name | RORγt Inverse agonist 6 | ||||||||||||
CAS | 1887161-80-9 | ||||||||||||
Formula | C28H29ClN6O5 | ||||||||||||
Molar Mass | 565.02 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Sato A, et al. Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists. ChemMedChem. 2019 Oct 28. |