WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H555401
CAS#: 610318-54-2 (free form)
Description: RGX-104, also known as SB 742881, is a liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
Hodoodo Cat#: H555401
Name: RGX-104 free form
CAS#: 610318-54-2 (free form)
Chemical Formula: C34H33ClF3NO3
Exact Mass: 595.21
Molecular Weight: 596.087
Elemental Analysis: C, 68.51; H, 5.58; Cl, 5.95; F, 9.56; N, 2.35; O, 8.05
Related CAS #: 610318-54-2 (free form) 610318-03-1 (HCl) 2648455-06-3 (zinc)
Synonym: Abequolixron; RGX-104 free form, RGX-104; RGX104; RGX 104; SB742881; SB-742881; SB 742881;
IUPAC/Chemical Name: (R)-2-[3-[3-[[2-Chloro-3-(trifluoromethyl)benzyl](2,2-diphenylethyl)amino]-3-methylpropoxy]phenyl]acetic acid
InChi Key: ZLJZDYOBXVOTSA-XMMPIXPASA-N
InChi Code: InChI=1S/C34H33ClF3NO3/c1-24(18-19-42-29-16-8-10-25(20-29)21-32(40)41)39(22-28-15-9-17-31(33(28)35)34(36,37)38)23-30(26-11-4-2-5-12-26)27-13-6-3-7-14-27/h2-17,20,24,30H,18-19,21-23H2,1H3,(H,40,41)/t24-/m1/s1
SMILES Code: O=C(O)CC1=CC=CC(OCC[C@H](N(CC2=CC=CC(C(F)(F)F)=C2Cl)CC(C3=CC=CC=C3)C4=CC=CC=C4)C)=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | 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, tumor cells and endothelial cells in the tumor microenvironment. This reverses immune evasion, enhances anti-tumor immune responses and inhibits proliferation of tumor cells. |
| In vitro activity: | RGX-104 remodels the acidic tumor microenvironment by transcriptional activation of ApoE to regress myeloid-derived suppressor cells' (MDSCs) activity, which neatly creates foreshadowing for intensifying pyroptosis. RNA-seq analysis of MRC at the cellular level reveals the intimate relationship between RGX-104 acting on LXR/ApoE axis and pyroptosis, where RGX-104 provides the prerequisite for pyroptosis participating in antitumor therapy. Reference: Adv Healthc Mater. 2022 Nov;11(21):e2201233. https://pubmed.ncbi.nlm.nih.gov/36049144/ |
| In vivo activity: | This study aimed to design a dual-pH-sensitivity conjugated micelle system (PAH/RGX-104@PDM/PTX) that could deliver RGX-104 and paclitaxel (PTX) to the perivascular region and tumor cells. Results suggest that the codelivery nanocarrier not only cause apoptosis of cancer cells but also regulate the tumor immune environment to ultimately enhance the antitumor effect of CTLs through MDSCs depletion. Reference: J Control Release. 2020 Jan 10;317:43-56. https://pubmed.ncbi.nlm.nih.gov/31758970/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100.0 | 167.76 |
The following data is based on the product molecular weight 596.09 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Qiu W, Su W, Xu J, Liang M, Ma X, Xue P, Kang Y, Sun ZJ, Xu Z. Immunomodulatory-Photodynamic Nanostimulators for Invoking Pyroptosis to Augment Tumor Immunotherapy. Adv Healthc Mater. 2022 Nov;11(21):e2201233. doi: 10.1002/adhm.202201233. Epub 2022 Sep 13. PMID: 36049144. 2. Liang H, Shen X. LXR activation radiosensitizes non-small cell lung cancer by restricting myeloid-derived suppressor cells. Biochem Biophys Res Commun. 2020 Jul 23;528(2):330-335. doi: 10.1016/j.bbrc.2020.04.137. Epub 2020 May 22. PMID: 32448508. 3. Wan D, Yang Y, Liu Y, Cun X, Li M, Xu S, Zhao W, Xiang Y, Qiu Y, Yu Q, Tang X, Zhang Z, He Q. Sequential depletion of myeloid-derived suppressor cells and tumor cells with a dual-pH-sensitive conjugated micelle system for cancer chemoimmunotherapy. J Control Release. 2020 Jan 10;317:43-56. doi: 10.1016/j.jconrel.2019.11.011. Epub 2019 Nov 20. PMID: 31758970. |
| In vitro protocol: | 1. Qiu W, Su W, Xu J, Liang M, Ma X, Xue P, Kang Y, Sun ZJ, Xu Z. Immunomodulatory-Photodynamic Nanostimulators for Invoking Pyroptosis to Augment Tumor Immunotherapy. Adv Healthc Mater. 2022 Nov;11(21):e2201233. doi: 10.1002/adhm.202201233. Epub 2022 Sep 13. PMID: 36049144. 2. Liang H, Shen X. LXR activation radiosensitizes non-small cell lung cancer by restricting myeloid-derived suppressor cells. Biochem Biophys Res Commun. 2020 Jul 23;528(2):330-335. doi: 10.1016/j.bbrc.2020.04.137. Epub 2020 May 22. PMID: 32448508. |
| In vivo protocol: | 1. Liang H, Shen X. LXR activation radiosensitizes non-small cell lung cancer by restricting myeloid-derived suppressor cells. Biochem Biophys Res Commun. 2020 Jul 23;528(2):330-335. doi: 10.1016/j.bbrc.2020.04.137. Epub 2020 May 22. PMID: 32448508. 2. Wan D, Yang Y, Liu Y, Cun X, Li M, Xu S, Zhao W, Xiang Y, Qiu Y, Yu Q, Tang X, Zhang Z, He Q. Sequential depletion of myeloid-derived suppressor cells and tumor cells with a dual-pH-sensitive conjugated micelle system for cancer chemoimmunotherapy. J Control Release. 2020 Jan 10;317:43-56. doi: 10.1016/j.jconrel.2019.11.011. Epub 2019 Nov 20. PMID: 31758970. |
1: Aravindhan K, Webb CL, Jaye M, Ghosh A, Willette RN, DiNardo NJ, Jucker BM.
Assessing the effects of LXR agonists on cellular cholesterol handling: a stable
isotope tracer study. J Lipid Res. 2006 Jun;47(6):1250-60. Epub 2006 Mar 27.
PubMed PMID: 16567856.
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K, Jucker B, Burgert M, Ma C, Marino JP, Collins JL, Macphee CH, Thompson SK,
Jaye M. Synthetic LXR agonists increase LDL in CETP species. J Lipid Res. 2005
Oct;46(10):2182-91. Epub 2005 Jul 16. PubMed PMID: 16024916.
