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RGX-104, also known as SB 742881, is a liver X receptor beta (LXR) agonist with potential immunomodulating and antineoplastic activities. RGX-104 modulates innate immunity via transcriptional activation of the ApoE gene.
Oral administration of RGX-104 selectively targets and binds to LXRbeta, thereby activating LXRbeta-mediated signaling, leading to the transcription of certain tumor suppressor genes and the downregulation of certain tumor promoter genes. This particularly activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in tumor cells and certain immune cells. This activates the innate immune system, resulting in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells.
| Molecular Weight | 596.08 |
| Formula | C34H33ClF3NO3 |
| CAS Number | 610318-54-2 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage | 2-8°C, protect from light, sealed |
| Related Liver X Receptor Products |
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GSK2033 is a potent LXR antagonist. |
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