A cell-permeable diaryl amide derived from T1317 (a known LXR agonist and retinoic acid receptor (ROR) inverse agonist) that acts as a highly selective agonist of RORalpha/gamma and does not exhibit affinity for FXR, LXRa and LXRb. Shown to stabilize p53 in cancer cells and increase the expression of p21 and PUMA. Induces apoptosis in hepatocellular carcinoma (HepG2) cells in a RORa and p53-dependent process. Also reported to increase the expression of Sox4 and REV-ERBa in HepG2 cells. Exhibits suitable pharmacokinetic properties with sustained plasma levels even after 8 hours following a single i.p. injection. Exposure to SR1078 Induces expression of glucose-6-phosphatase and fibroblast growth factor 21 in murine models (10mg/kg/i.p.).
Storage and Stability:Store at -20°C under inert atmosphere. Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
