SR 1903 - CAS 1414248-06-8

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR) .1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1 in RAW 264.7 cells. SR 1903 (20 mg/kg twice per day) reduces severity score in a mouse model of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.

ROR, Liver X Receptor, Others, PPAR

DNA Damage/DNA Repair, Others, Metabolism

1414248-06-8

C27H27F6N3O

523.51

CC1=C(C2=CC=C(C(C(F)(F)F)(C(F)(F)F)O)C=C2)C=CC(CN3CCN(CC=4C=CN=CC4)CC3)=C1

-20°C

Ice Packs

Small Compound