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RGX-104

Cat. No. M10589
RGX-104 Structure
Synonym:

SB 742881; RGX-104 free form

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Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Masoud F Tavazoie, et al. Cell. LXR/ApoE Activation Restricts Innate Immune Suppression in Cancer

[2] Karpagam Aravindhan, et al. J Lipid Res. Assessing the effects of LXR agonists on cellular cholesterol handling: a stable isotope tracer study

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Keywords: RGX-104, SB 742881; RGX-104 free form supplier, Liver X Receptor, inhibitors, activators


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