PA 452

Pricing Availability   Qty
Description: RXR antagonist
Chemical Name: 2-[[3-(Hexyloxy)-5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl]methylamino]-5-pyrimidinecarboxylic acid
Purity: ≥98% (HPLC)
Citations (2)
Literature (1)

Biological Activity for PA 452

PA 452 is an RXR antagonist (pA2 = 7.11). Triggers dissociation of RXR tetramers. Attenuates cell proliferation and induces apoptosis in MCF-7 breast cancer cells.

Technical Data for PA 452

M. Wt 439.59
Formula C26H37N3O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 457657-34-0
PubChem ID 9803242
Smiles CC1(C)C2=C(C=C(N(C3=NC=C(C(O)=O)C=N3)C)C(OCCCCCC)=C2)C(C)(C)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PA 452

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 43.96 100
ethanol 4.4 10

Preparing Stock Solutions for PA 452

The following data is based on the product molecular weight 439.59. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.27 mL 11.37 mL 22.75 mL
5 mM 0.45 mL 2.27 mL 4.55 mL
10 mM 0.23 mL 1.14 mL 2.27 mL
50 mM 0.05 mL 0.23 mL 0.45 mL

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References for PA 452

References are publications that support the biological activity of the product.

Yasmin et al (2010) Inhibition of mammary carcinoma cell growth by RXR is mediated by the receptor's oligomeric switch. J.Mol.Biol. 397 1121 PMID: 20188110

Takahashi et al (2002) Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions. J.Med.Chem. 45 3327 PMID: 12139443

Nakayama et al (2011) Discovery of a potent retinoid X receptor antagonist structurally closely related to RXR agonist NEt-3IBIB. J.Med.Chem.Lett 2 896 PMID: 24900278

If you know of a relevant reference for PA 452, please let us know.

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Keywords: PA 452, PA 452 supplier, PA452, RXR, tetramers, retinoid, X, receptors, antagonists, Retinoid, Receptor, 5086, Tocris Bioscience

2 Citations for PA 452

Citations are publications that use Tocris products. Selected citations for PA 452 include:

Yuan et al (2018) A Chimeric Humanized Mouse Model by Engrafting the Human Induced Pluripotent Stem Cell-Derived Hepatocyte-Like Cell for the Chronic Hepatitis B Virus Infection. Front Microbiol 9 908 PMID: 29867819

Wang et al (2017) Retinoic acid inhibits white adipogenesis by disrupting GADD45A-mediated Zfp423 DNA demethylation. J Mol Cell Biol 9 338 PMID: 28992291

Do you know of a great paper that uses PA 452 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Retinoid Receptors Scientific Review

Retinoid Receptors Scientific Review

Written by Alexander Moise, this review summarizes the nature of retinoid receptors, their isotype and isoform variants and modulation of retinoid signaling. Compounds available from Tocris are listed.