WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206942
CAS#: 610318-03-1 (HCl)
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#: H206942
Name: RGX-104 HCl
CAS#: 610318-03-1 (HCl)
Chemical Formula: C34H34Cl2F3NO3
Exact Mass: 0.00
Molecular Weight: 632.560
Elemental Analysis: C, 64.56; H, 5.42; Cl, 11.21; F, 9.01; N, 2.21; O, 7.59
Related CAS #: 610318-54-2 (free form) 610318-03-1 (HCl) 2648455-06-3 (zinc)
Synonym: Abequolixron, RGX-104 hydrochloride; RGX-104 HCl; 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 hydrochloride
InChi Key: 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.[H]Cl
InChi Code: InChI=1S/C34H33ClF3NO3.ClH/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);1H/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.[H]Cl
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: >2 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: LXRbeta, a member of the oxysterol receptor family, which is in the nuclear receptor family of transcription factors, plays a key role in cholesterol transport, glucose metabolism and the modulation of inflammatory responses; activation of LXRbeta suppresses tumor cell invasion, angiogenesis, tumor progression, and metastasis in a variety of tumor cell types. The expression of the ApoE protein becomes silenced in human cancers as they grow, become invasive, and metastasize; ApoE silencing is related to reduced survival in cancer patients. The LXR-ApoE pathway regulates the ability of cancers to evade the immune system and recruit blood vessels.
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 632.56 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: | |
| In vitro protocol: | |
| In vivo protocol: |
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.
2: Groot PH, Pearce NJ, Yates JW, Stocker C, Sauermelch C, Doe CP, Willette RN,
Olzinski A, Peters T, d'Epagnier D, Morasco KO, Krawiec JA, Webb CL, Aravindhan
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.
