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CD 2665

Catalog No.
B7501
Selective RARβ/γ antagonist
Grouped product items
SizePriceStock Qty
5mg
$146.00
Ship with 5-10 days
10mg
$243.00
Ship with 5-10 days
50mg
$947.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

CD 2665 is a retinoic acid receptor β (RARβ) / RARγ antagonist [1] [2] [3] with binding Kd values of 306 nM and 110 nM to RARβ and RARγ, respectively [3].

Retinoic acid receptors include RARα, RARβ and RARγ. They are able to bind 9-cis and all-trans stereoisomers of retinoic acid (RA) [1], and mediate RA signal as transcription factors [2].

CD 2665 (1 µM) did not antagonize the luciferase activity induced by 9-cis- or all-trans-RA in HiB5 cells, but partially blocked the luciferase activity in 3XbRARE-Luc-transfected cells induced by CD 666 (a RARγ-selective agonist, 100 nM). CD 2665 at 1 µM reduced the viable cell number to about 60% level of vehicle-treated cells. CD 2665 (1 µM) clearly antagonized the increase in cell number resulted from the treatment with CD 666 (100 nM) [4].

The biosynthesis of retinoic acid can also be disordered by chronic ethanol consumption. CD 2665 administration did not modify blood alcohol levels in alcohol-treated mice, but totally reversed the impairment of spontaneous alternation rates resulted from alcohol consumption. Administration with CD2665 for 22 days in alcohol-treated mice significantly decreased both mRNA expression and enzymatic activity of tTG (a retinoic acid-target gene) and normalized the expression levels to the level in control mice [2].

References:
[1].  Yasmin Marikar, ZengQuan Wang, Elizabeth A. Duell, et al. Retinoic Acid Receptors Regulate Expression of Retinoic Acid 4-Hydroxylase that Specifically Inactivates All-Trans Retinoic Acid in Human Keratinocyte HaCaT Cells. The Journal of Investigative Dermatology, 1998, 111(3):434-439.
[2].  Serge Alfos, Catherine Boucheron, Véronique Pallet, et al. A Retinoic Acid Receptor Antagonist Suppresses Brain Retinoic Acid Receptor Overexpression and Reverses a Working Memory Deficit Induced by Chronic Ethanol Consumption in Mice. Alcohol Clin Exp Res., 2001, 25(10): 1506-1514.
[3].  Zsuzsa Szondy, Uwe Reichert, Jean-Michel Bernardon, et al. Inhibition of activation-induced apoptosis of thymocytes by all-trans- and 9-cis-retinoic acid is mediated via retinoic acid receptor α. Biochem. J., 1998, 331:767-774.
[4].  Jean-Ju Chung, Sehyung Cho, Yunhee Kim Kwon, et al. Activation of retinoic acid receptor γ induces proliferation of immortalized hippocampal progenitor cells. Molecular Brain Research, 2000, 83:52-62.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt486.6
Cas No.170355-78-9
FormulaC31H34O5
SolubilitySoluble in DMSO
Chemical Name4-(7-((1s,3R,5S,7s)-adamantan-1-yl)-6-((2-methoxyethoxy)methoxy)naphthalen-2-yl)benzoic acid
SDFDownload SDF
Canonical SMILESOC(C1=CC=C(C=C1)C2=CC=C3C(C=C(C(OCOCCOC)=C3)[[email protected]]4(C[[email protected]](C5)C6)C[[email protected]@H]5C[[email protected]]6C4)=C2)=O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

CD 2665