Date published: 2025-10-16

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LG 100754 (CAS 180713-37-5)

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Alternate Names:
(2E,4E,6Z)-3-Methyl-7-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-propoxy-3-naphthalenyl)-2,4,6-octatrienoic acid
Application:
LG 100754 is an agonist of RXR:PPARγ that enhances ligand binding activity
CAS Number:
180713-37-5
Purity:
≥98%
Molecular Weight:
396.56
Molecular Formula:
C26H36O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Available in US only.
* Refer to Certificate of Analysis for lot specific data.

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LG 100754 is an agonist of RXR:PPARgamma that enhances ligand binding activity with PPARgamma. This compound has been found to contain selectivity over other permissive heterodimers such as RXR:LXRalpha and RXR:BAR/FXR. In cotransfection assays, LG 100754 additionally activates RXR:RAR and RXR:PPARalpha heterodimers. Also as an antagonist against RXR homodimers.


LG 100754 (CAS 180713-37-5) References

  1. Retinoid X receptor-antagonistic diazepinylbenzoic acids.  |  Ebisawa, M., et al. 1999. Chem Pharm Bull (Tokyo). 47: 1778-86. PMID: 10748721
  2. HIV protease inhibitors stimulate hepatic triglyceride synthesis.  |  Lenhard, JM., et al. 2000. Arterioscler Thromb Vasc Biol. 20: 2625-9. PMID: 11116063
  3. Existence of retinoic acid-receptor-independent retinoid X-receptor-dependent pathway in myeloid cell function.  |  Hida, T., et al. 2001. Jpn J Pharmacol. 85: 60-9. PMID: 11243576
  4. The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo.  |  Cesario, RM., et al. 2001. Mol Endocrinol. 15: 1360-9. PMID: 11463859
  5. The antidiabetic agent LG100754 sensitizes cells to low concentrations of peroxisome proliferator-activated receptor gamma ligands.  |  Forman, BM. 2002. J Biol Chem. 277: 12503-6. PMID: 11877384
  6. Retinoid signalling and gene expression in neuroblastoma cells: RXR agonist and antagonist effects on CRABP-II and RARbeta expression.  |  Hewson, QC., et al. 2002. J Cell Biochem. 87: 284-91. PMID: 12397610
  7. The use of in vitro peptide binding profiles and in silico ligand-receptor interaction profiles to describe ligand-induced conformations of the retinoid X receptor alpha ligand-binding domain.  |  Folkertsma, S., et al. 2007. Mol Endocrinol. 21: 30-48. PMID: 17038419
  8. The 'Phantom Effect' of the Rexinoid LG100754: structural and functional insights.  |  Sato, Y., et al. 2010. PLoS One. 5: e15119. PMID: 21152046
  9. Protective effects of retinoid x receptors on retina pigment epithelium cells.  |  Ayala-Peña, VB., et al. 2016. Biochim Biophys Acta. 1863: 1134-45. PMID: 26883505
  10. Antagonist-perturbation mechanism for activation function-2 fixed motifs: active conformation and docking mode of retinoid X receptor antagonists.  |  Tsuji, M. 2017. J Comput Aided Mol Des. 31: 577-585. PMID: 28534193
  11. Regulation of RXR-RAR Heterodimers by RXR- and RAR-Specific Ligands and Their Combinations.  |  le Maire, A., et al. 2019. Cells. 8: PMID: 31694317
  12. Protection against influenza-induced Acute Lung Injury (ALI) by enhanced induction of M2a macrophages: possible role of PPARγ/RXR ligands in IL-4-induced M2a macrophage differentiation.  |  Gopalakrishnan, A., et al. 2022. Front Immunol. 13: 968336. PMID: 36052067
  13. The phantom ligand effect: allosteric control of transcription by the retinoid X receptor.  |  Schulman, IG., et al. 1997. Genes Dev. 11: 299-308. PMID: 9030683
  14. Retinoid signaling is required for the establishment of a ZPA and for the expression of Hoxb-8, a mediator of ZPA formation.  |  Lu, HC., et al. 1997. Development. 124: 1643-51. PMID: 9165113

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

LG 100754, 5 mg

sc-361231
5 mg
$134.00
US: Only available in the US

LG 100754, 25 mg

sc-361231A
25 mg
$544.00
US: Only available in the US