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CD 3254

Catalog No.
B7352
RXRα agonist,potent and selective
Grouped product items
SizePriceStock Qty
5mg
$131.00
Ship with 5-10 days
10mg
$209.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

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Background

CD3254 is a potent and selective agonist of Retinoid X receptors (RXRα).

Retinoid X receptors (RXRs) are nuclear receptors that act as ligand-dependent transcription factors and function as the homodimer or as heterodimers with other nuclear receptors, such as retinoic acid receptors (RARs), peroxisome proliferator-activated receptors (PPARs), or liver X receptors (LXRs). RXR plays essential roles in the regulation of glucose metabolism, lipid metabolism and immune response. Retinoid X receptors (RXRs) contains three family members including RARα, RARβ or RARγ receptors. RXRα belongs to the NR2B nuclear receptor family and primarily expressed in the liver, intestines, kidneys, and epidermis.

CD3254 and its’ analogue bexarotene have been reported as a treatment for cutaneous T-cell lymphoma (CTCL), despite the fact that treatment with CD3254 can evoke reactions by disturbing other RXR-heterodimer receptor pathways. Of the seven displayed novel exacerbates, all analogs animate RXR-controlled translation in mammalian 2 hybrid and RXRE-interceded tests, have equivalent or hoisted natural action in view of EC50 profiles, and hold comparative or enhanced apoptotic movement in CTCL assays contrasted with CD3254. Every single novel compound show selectivity for RXR and insignificant hybrid onto the retinoic corrosive receptor (RAR) contrasted with all-trans-retinoic corrosive, with select analogs likewise decreasing hindrance of other RXR-subordinate pathways (e.g., VDR-RXR) [1].

In vivo, CD3254 induced the phenotypes of malformations after 5 days exposure at low concentration (20 μg/l) to those after the 1st d exposure at high concentrations (50 and 100 μg/L) [2].

References:
Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene) and (E)-3-(3-(1,2,3,4-tetrahydro-1,1,4,4,6-pentamethylnaphthalen-7-yl)-4-hydroxyphenyl)acrylic acid (CD3254).  J Med Chem. 2013 Nov 14;56(21):8432-54. doi: 10.1021/jm4008517. Epub 2013 Nov 1.
Divergent teratogenicity of agonists of retinoid X receptors in embryos of zebrafish (Danio rerio).  Ecotoxicology. 2012 Jul;21(5):1465-75. doi: 10.1007/s10646-012-0900-9. Epub 2012 Apr 10.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt364.48
Cas No.196961-43-0
FormulaC24H28O3
SolubilitySoluble in DMSO
Chemical Name(E)-3-(4-hydroxy-3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)phenyl)acrylic acid
SDFDownload SDF
Canonical SMILESOC1=CC=C(/C=C/C(O)=O)C=C1C2=C(C)C=C3C(C)(C)CCC(C)(C)C3=C2
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

CD 3254