Inverse agonist activity at APC-labeled RORgammat LBD (unknown origin) assessed as inhibition of europium-labeled co-activator SRC1 recruitment incubated for 1 hr by FRET assay
Inverse agonist activity at APC-labeled RORgammat LBD (unknown origin) assessed as inhibition of europium-labeled co-activator SRC1 recruitment incubated for 1 hr by FRET assay relative to control
Inverse agonist activity at RORgammat in mouse CD4+ T cells assessed as inhibition of differentiation into Th17 cells by measuring IL-17 production by flow cytometry
Inverse agonist activity at RORgammat in mouse CD4+ T cells assessed as inhibition of differentiation into Th17 cells by measuring IL-17 production by flow cytometry relative to control
Metabolic stability in CD-1 mouse liver microsomes assessed as parent compound remaining at 1 uM measured at 60 mins in presence of NADPH by LC-MS/MS analysis
Antiinflammatory activity against imiquimod-induced psoriasis in ip dosed BALB/c mouse model assessed as reduction in clinical severity administered once daily for 12 days
Antiinflammatory activity against imiquimod-induced psoriasis BALB/c mouse model assessed as reduction in ear thickness at 10 to 50 mg/kg, ip administered once daily for 12 days by hematoxylin and eosin staining based analysis
Antiinflammatory activity against imiquimod-induced psoriasis BALB/c mouse model assessed as body weight loss at 50 mg/kg, ip administered once daily for 12 days (Rvb = 19.94 +/- 0.78 g)
Antiinflammatory activity against imiquimod-induced psoriasis BALB/c mouse model assessed as body weight loss at 10 mg/kg, ip administered once daily for 12 days (Rvb = 19 +/- 0.64 g)
Antiinflammatory activity against imiquimod-induced psoriasis BALB/c mouse model assessed as body weight loss at 2 mg/kg, ip administered once daily for 12 days (Rvb = 19.89 +/- 1.16 g)
Antiinflammatory activity against imiquimod-induced psoriasis BALB/c mouse model assessed as body weight loss at 0.4 mg/kg, ip administered once daily for 12 days (Rvb = 19.71 +/- 0.92 g)
Antiinflammatory activity against imiquimod-induced psoriasis BALB/c mouse model assessed as inhibition of back skin erythema at 0.4 mg/kg, ip administered once daily for 12 days
Antiinflammatory activity against imiquimod-induced psoriasis BALB/c mouse model assessed as inhibition of back skin scaling at 0.4 mg/kg, ip administered once daily for 12 days