RGX-104

An LXRa and LXRß agonist, induces recruitment of an SRC-1 fragment in cell-free FRET-based assays (EC50s = 74 and 25 nM for LXRa and LXRß, respectively), induces cholesterol efflux in RAW 264.7 macrophages (EC50 = 17 nM), increases plasma levels of VLDL, LDL, and triglycerides in hamsters at 10 mg/kg twice per day and decreases plasma levels of HDL in the same animals at 30 mg/kg twice per day, increases hepatic levels of triglycerides in hamsters at 10 or 30 mg/kg per day, increases serum levels of ApoB in cynomolgus monkeys at 10 mg/kg per day, decreases PHMG-induced increases in lung tissue levels of fibronectin and collagen 1A1 and BALF levels of foam macrophages in a mouse model of pulmonary fibrosis at 20 mg/kg per day. Formulation: A solid. InChI: InChI=1S/C34H33ClF3NO3/c1-24(18-19-42-29-16-8-10-25(20-29)21-32(40)41)39(22-28-15-9-17-31(33(28)35)34(36,37)38)23-30(26-11-4-2-5-12-26)27-13-6-3-7-14-27/h2-17,20,24,30H,18-19,21-23H2,1H3,(H,40,41)/t24-/m1/s1. InChIKey: ZLJZDYOBXVOTSA-XMMPIXPASA-N. SMILES: ClC(C(C(F)(F)F)=CC=C1)=C1CN(CC(C2=CC=CC=C2)C3=CC=CC=C3)[C@@H](CCOC4=CC(CC(O)=O)=CC=C4)C