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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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| Rovazolac
Rovazolac is a liver x receptor (LXR) modulator, which can be used in the study of immune system disorders and atopic dermatitis. |
| GW6340
GW6340 is an intestinal-specific LXR agonist. |
| Larsucosterol
Larsucosterol is an endogenous sulfated oxysterol and a potent hepatic X receptor (LXR) and DNA methylase (DNMTS) antagonist that regulates endogenous lipogenesis as well as inhibits cholesterol biosynthesis by lowering mRNA levels and inhibiting SREBP-1 activation. May be used in studies related to psoriasis. |
| 24(S)-Hydroxycholesterol
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators. |
| GW3965
GW3965 is a potent, selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively. |
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