PA-452

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 562909

CAS#: 457657-34-0

Description: PA-452 is an RXR antagonist.


Price and Availability

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Price

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PA-452 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 562909
Name: PA-452
CAS#: 457657-34-0
Chemical Formula: C26H37N3O3
Exact Mass: 439.2835
Molecular Weight: 439.6
Elemental Analysis: C, 71.04; H, 8.48; N, 9.56; O, 10.92


Synonym: PA-452; PA 452; PA452;

IUPAC/Chemical Name: 2-((3-(hexyloxy)-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalen-2-yl)(methyl)amino)pyrimidine-5-carboxylic acid

InChi Key: JJUUTJCZMGZJDZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H37N3O3/c1-7-8-9-10-13-32-22-15-20-19(25(2,3)11-12-26(20,4)5)14-21(22)29(6)24-27-16-18(17-28-24)23(30)31/h14-17H,7-13H2,1-6H3,(H,30,31)

SMILES Code: OC(C1=CN=C(N(C)C2=C(OCCCCCC)C=C3C(C(C)(C)CCC3(C)C)=C2)N=C1)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Xia Y, Carpentier A, Cheng X, Block PD, Zhao Y, Zhang Z, Protzer U, Liang TJ. Human stem cell-derived hepatocytes as a model for hepatitis B virus infection, spreading and virus-host interactions. J Hepatol. 2017 Mar;66(3):494-503. doi: 10.1016/j.jhep.2016.10.009. Epub 2016 Oct 14. PubMed PMID: 27746336; PubMed Central PMCID: PMC5316493.

2: German OL, Monaco S, Agnolazza DL, Rotstein NP, Politi LE. Retinoid X receptor activation is essential for docosahexaenoic acid protection of retina photoreceptors. J Lipid Res. 2013 Aug;54(8):2236-46. doi: 10.1194/jlr.M039040. Epub 2013 May 30. PubMed PMID: 23723389; PubMed Central PMCID: PMC3708373.

3: Nakayama M, Yamada S, Ohsawa F, Ohta Y, Kawata K, Makishima M, Kakuta H. Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related to RXR Agonist NEt-3IB. ACS Med Chem Lett. 2011 Sep 27;2(12):896-900. doi: 10.1021/ml200197e. eCollection 2011 Dec 8. PubMed PMID: 24900278; PubMed Central PMCID: PMC4018080.

4: Suzuki K, Takahashi K, Nishimaki-Mogami T, Kagechika H, Yamamoto M, Itabe H. Docosahexaenoic acid induces adipose differentiation-related protein through activation of retinoid x receptor in human choriocarcinoma BeWo cells. Biol Pharm Bull. 2009 Jul;32(7):1177-82. PubMed PMID: 19571381.

5: Dillard AC, Lane MA. Retinol decreases beta-catenin protein levels in retinoic acid-resistant colon cancer cell lines. Mol Carcinog. 2007 Apr;46(4):315-29. PubMed PMID: 17219422.

6: Honda M, Hamazaki TS, Komazaki S, Kagechika H, Shudo K, Asashima M. RXR agonist enhances the differentiation of cardiomyocytes derived from embryonic stem cells in serum-free conditions. Biochem Biophys Res Commun. 2005 Aug 12;333(4):1334-40. PubMed PMID: 15982638.

7: Varley CL, Stahlschmidt J, Smith B, Stower M, Southgate J. Activation of peroxisome proliferator-activated receptor-gamma reverses squamous metaplasia and induces transitional differentiation in normal human urothelial cells. Am J Pathol. 2004 May;164(5):1789-98. PubMed PMID: 15111325; PubMed Central PMCID: PMC1615665.

8: Iwata M, Eshima Y, Kagechika H. Retinoic acids exert direct effects on T cells to suppress Th1 development and enhance Th2 development via retinoic acid receptors. Int Immunol. 2003 Aug;15(8):1017-25. PubMed PMID: 12882839.