SR 1903

SR 1903 is a modulator of retinoic acid receptor-related orphan receptor gamma (RORgamma) and liver X receptor (LXR). It is an inverse agonist of RORgamma (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor gamma (PPARgamma, 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.Formal Name: 2'-methyl-4'-[[4-(4-pyridinylmethyl)-1-piperazinyl]methyl]-alpha,alpha-bis(trifluoromethyl)-[1,1'-biphenyl]-4-methanol. CAS Number: 1414248-06-8. Molecular Formula: C27H27F6N3O. Formula Weight: 523.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, Ethanol: 10 mg/ml. lambdamax: 249 nm. SMILES: CC1=C(C2=CC=C(C(O)(C(F)(F)F)C(F)(F)F)C=C2)C=CC(CN(CC3)CCN3CC4=CC=NC=C4)=C1. InChi Code: InChI=1S/C27H27F6N3O/c1-19-16-21(18-36-14-12-35(13-15-36)17-20-8-10-34-11-9-20)2-7-24(19)22-3-5-23(6-4-22)25(37,26(28,29)30)27(31,32)33/h2-11,16,37H,12-15,17-18H2,1H3. InChi Key: HSUQYJQLSYQEOB-UHFFFAOYSA-N.