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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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Liver X Receptor Products |
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| BMS-779788
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ. |
| RGX-104 hydrochloride
RGX-104 hydrochloride is a small-molecule LXR (liver X receptor) agonist that modulates innate immunity via transcriptional activation of the ApoE gene. |
| Iristectorigenin B
Iristectorigenin B is a liver X receptor (LXR) modulator, which stimulates the transcriptional activity of both LXR-α and LXR-β. |
| Yamogenin
Yamogenin (Diosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. |
| SR9238
SR9238 is a liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively. |
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