1. Metabolic Enzyme/Protease
  2. 15-PGDH
  3. 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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CAY10397

CAY10397 Chemical Structure

CAS No. : 78028-01-0

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Description

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[1][2].

In Vitro

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.

In Vivo

CAY10397 (100 mg/kg; i.g.; every other day) blocks the selenium-dependent protective effects against DSS (HY-116282C)-induced colitis, exacerbating inflammation, reducing gut barrier function, and inhibiting 15-PGDH activity[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Administration: oral gavage; every alternate day; starting at day -1 relative to DSS treatment
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.
Molecular Weight

328.32

Formula

C17H16N2O5

CAS No.
SMILES

OC1=C(C=C(C=C1)/N=N/C2=CC=C(C=C2)C(OCC)=O)CC(O)=O

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CAY10397
Cat. No.:
HY-119973
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