RGX-104

RGX-104 is an agonist of liver X receptor a (LXRa) and LXRß.¹ It induces recruitment of a steroid receptor coactivator 1 (SRC-1) fragment in cell-free FRET-based assays (EC₅₀s = 74 and 25 nM for LXRa and LXRß, respectively). RGX-104 induces cholesterol efflux in RAW 264.7 macrophages (EC₅₀ = 17 nM). It increases plasma levels of VLDL, LDL, and triglycerides in hamsters when administered at a dose of 10 mg/kg twice per day and decreases plasma levels of HDL in the same animals at 30 mg/kg twice per day.² RGX-104 (10 or 30 mg/kg per day) increases hepatic levels of triglycerides in hamsters. It increases serum levels of apolipoprotein B (ApoB) in cynomolgus monkeys when administered at a dose of 10 mg/kg per day. RGX-104 (20 mg/kg per day) decreases lung tissue levels of fibronectin and collagen 1A1 and bronchoalveolar lavage fluid (BALF) levels of foam macrophages in a mouse model of pulmonary fibrosis induced by polyhexamethylene guanidine (PHMG).³

WARNING This product is not for human or veterinary use.

1. Marino, J.P., Jr., Kallander, L.S., Ma, C., et al. The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages. Bioorg. Med. Chem. Lett. 19(19), 5617-5621 (2009).

2. Groot, P.H.E., Pearce, N.J., Yates, J.W., et al. Synthetic LXR agonists increase LDL in CETP species. J. Lipid Res. 46(10), 2182-2191 (2005).

3. Sun, H., Yan, Z., Sun, J., et al. Polyhexamethylene guanidine accelerates the macrophage foamy formation mediated pulmonary fibrosis. Ecotoxicol. Environ. Saf. 272, 116084 (2024).