A selective RXR agonist
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CD3254

Item No. 20870

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[4-hydroxy-3-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)phenyl]-2-propenoic acid
CAS Number
196961-43-0
Molecular Formula
C24H28O3
Formula Weight
364.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2)(1:8): 0.11 mg/mlEthanol: 20 mg/ml
λmax
210, 316 nm
SMILES
CC1(C)C2=C(C=C(C)C(C3=C(O)C=CC(/C=C/C(O)=O)=C3)=C2)C(C)(C)CC1
InChi Code
InChI=1S/C24H28O3/c1-15-12-19-20(24(4,5)11-10-23(19,2)3)14-17(15)18-13-16(6-8-21(18)25)7-9-22(26)27/h6-9,12-14,25H,10-11H2,1-5H3,(H,26,27)/b9-7+
InChi Key
DYLLZSVPAUUSSB-VQHVLOKHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $37

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    5 mg

    $136

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    10 mg

    $235

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    Product Description

    CD3254 is a selective agonist of the retinoid X receptors (RXRs; EC50 = ~10 nM for human RXRβ) that is without effect on retinoic acid receptors (RARs).1,2 It stimulates the recruitment of the nuclear receptor interaction domain of the TRAP220 coactivator to RXRα/RARβ heterodimers in vitro.3 CD3254 also enhances the recruitment of the PPARγ coactivator 1α, PGC-1α, to RXRα/PPARγ heterodimers.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nahoum, V., Pérez, E., Germain, P., et al. Modulators of the structural dynamics of the retinoid X receptor to reveal receptor function. Proc. Natl. Acad. Sci. USA 104(44), 17323-17328 (2007).

    2. Jurutka, P.W., Kaneko, I., Yang, J., et al. 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. 56(21), 8432-8454 (2013).

    3. Pogenberg, V., Guichou, J.-F., Vivat-Hannah, V., et al. Characterization of the interaction between retinoic acid receptor/retinoid X receptor (RAR/RXR) heterodimers and transcriptional coactivators through structural and fluorescence anisotropy studies. The Journal of Biological Chemisty 280(2), 1625-1633 (2005).

    4. le Maire, A., Grimaldi, M., Roecklin, D., et al. Activation of RXR-PPAR heterodimers by organotin environmental endocrine disruptors. EMBO reports 10(4), 367-373 (2009).