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NRX 194204
- NRX 4204 - VTP 194204 - AGN 194204 - AGN 4204
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C24H32O2
- MW: 352.51
Description
Highly potent and specific RXR agonist (Kd values 0.4 nM, 3.6 nM, and 3.8 nM for RXRα, RXRβ, and RXRγ, respectively) devoid of any RAR activity (Kd values >30 µM for RARα, RARβ, and RARγ). NRX 194204 blocked the ability of lipopolysaccharide and TNFα to induce the release of nitric oxide and IL6 and the degradation of IKBα in RAW264.7 macrophage-like cells. NRX194204 prevents carcinogenesis in both the lung and mammary gland, and enhances the ability of ligands for PPARs or cytotoxic drugs, including cisplatin and 5-flurouracil, to inhibit proliferation and induce apoptosis in breast and pancreatic cancer cell lines.
More Information
| Parent CAS No. | 220619-73-8 |
|---|---|
| Chemical Name | (2E,4E)-3-Methyl-5-((1S,2S)-2-methyl-2-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopropyl)penta-2,4-dienoic acid |
| SMILES | C1C(C)(C)C2C=C([C@@]3(C)C[C@@]3([H])/C=C/C(/C)=C/C(=O)O)C=CC=2C(C)(C)C1 |&1:7,10,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C24H32O2/c1-16(13-21(25)26)7-8-18-15-24(18,6)17-9-10-19-20(14-17)23(4,5)12-11-22(19,2)3/h7-10,13-14,18H,11-12,15H2,1-6H3,(H,25,26)/b8-7+,16-13+/t18-,24-/m1/s1 |
| InChiKey | BOOOLEGQBVUTKC-NVQSDHBMSA-N |
| CID | 9863341 |
| Short Description | RXR agonist |
References
- K. Liby et al. A new rexinoid, NRX194204, prevents carcinogenesis in both the lung and mammary gland. Clin Cancer Res. 2007 Oct 15;13(20):6237-43.
- V. Vuligonda et al. Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes. J Med Chem. 2001 Jul 5;44(14):2298-303.
- R. AS Chandraratna et al. Treatment with retinoid X receptor agonist IRX4204 ameliorates experimental autoimmune encephalomyelitis. Am J Transl Res. 2016; 8(2): 1016–1026.
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