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RGX-104

Cat. No. M10589
RGX-104 Structure
Synonym:

SB 742881; RGX-104 free form

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Quality Control
  • Current batch:
  • Purity >99.5%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 596.08
Formula C34H33ClF3NO3
CAS Number 610318-54-2
Purity >99.5%
Solubility DMSO 90 mg/mL
Storage 2-8°C, protect from light, sealed
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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RGX-104 hydrochloride

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

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