CAY10397
CAY10397 is a selective and orally active 15-hydroxyprostaglandin dehydrogenase (15-PGDH) inhibitor. CAY10397 can inhibit 15-PGDH-dependent endogenous metabolite production. CAY10397 blocks the selenium-dependent protective in inflammation. CAY10397 can be used for the research of colitis.
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- No. CAS: 78028-01-0
- Fòrmula: C17H16N2O5
- Peso molecular:328.32
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
CAY10397 (50 μM; 10 min) potently inhibits 15-PGDH activity in LoVo cell lysates, reducing formation of 15-PGDH-dependent metabolites including 11-oxo-ETE by 92%[1].
CAY10397 (50 μM; 10 min) does not alter levels of 15-PGDH precursor metabolites in HCA-7 cell lysates, which express negligible 15-PGDH[1].
CAY10397 inhibits the activity of purified human recombinant 15-PGDH[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS-induced acute colitis mice model
C57BL/6 (male, 3 weeks old, maintained on 0.4 ppm selenium diet for 10-12 weeks)[2] -
Dosage:100 mg/kg
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Administration:oral gavage; every alternate day; starting at day -1 relative to DSS treatment
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Result:Blocked the Se-mediated inhibition of colonic expression of TNF-α, IL-1β, IFN-
γ and COX-2.
Significantly reduced colonic expression of the anti-inflammatory/barrier-protective gene Muc-2 relative to vehicle controls.
Significantly increased colonic histopathological scores relative to vehicle controls.
Significantly reduced colonic 15-PGDH specific activity relative to vehicle controls.
Chemical Information
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No. CAS 78028-01-0
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Peso molecular 328.32
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Fòrmula C17H16N2O5
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SMILES
OC1=C(C=C(C=C1)/N=N/C2=CC=C(C=C2)C(OCC)=O)CC(O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Liu X, et al. 11-Oxoeicosatetraenoic acid is a cyclooxygenase-2/15-hydroxyprostaglandin dehydrogenase-derived antiproliferative eicosanoid. Chem Res Toxicol. 2011;24(12):2227-2236. [Content Brief]
[2]. Kaushal N, et al. Crucial role of macrophage selenoproteins in experimental colitis. J Immunol. 2014;193(7):3683-3692. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CAY10397 Related Classifications
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