1. Metabolic Enzyme/Protease Immunology/Inflammation
  2. Epoxide Hydrolase COX
  3. COX-2/sEH-IN-1

COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks.

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COX-2/sEH-IN-1 Chemical Structure

COX-2/sEH-IN-1 Chemical Structure

CAS No. : 2474977-38-1

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Description

COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks[1].

IC50 & Target

sEH

0.40 nM (IC50)

COX-2

1.24 μM (IC50)

COX-1

8.72 μM (IC50)

In Vivo

COX-2/sEH-IN-1 (Compound 9c) (10 mg/kg; p.o.; once) exhibits analgesic activity[1].
COX-2/sEH-IN-1 (50 mg/kg; p.o.; once) shows high anti-inflammatory activity[1].
COX-2/sEH-IN-1 (100 mg/kg; p.o.; 2 weeks) affords a perfect cardio-protection and less cardiovascular liabilities[1].

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

Animal Model: Albino mice (20-30 g)[1]
Dosage: 10 mg/kg
Administration: Oral administration, once
Result: Exhibited analgesic activity with 65.67% inhibition in the number of writhing.
Animal Model: Albino rats (120-150 g), carrageenan-induced paw edema model[1]
Dosage: 50 mg/kg
Administration: Oral administration, once
Result: Showed high anti-inflammatory activity with edema inhibition of 64.06%, 95.82%, and 98.15% at 1, 3, 5 h, respectively.
Animal Model: Adult male albino Wister rats (170-200 g)[1]
Dosage: 100 mg/kg
Administration: Oral administration, 2 weeks
Result: Exhibited a significant lowering in Troponine-I, LDH and CK-MB levels when compared to celecoxib treated group. Showed remarkably decrease in TNF-α concentration compared to the celecoxib induced cardio-toxicity group. Restored heart GSH level and significantly increased PGI2 level compared to celecoxib group. Showed mild decongestant and mild edema on cardiac blood vessels and showed more or less normal muscle bundles.
Molecular Weight

501.48

Formula

C23H18F3N5O3S

CAS No.
SMILES

NS(=O)(C1=CC=C(C=C1)N2N=C(C=C2C3=CC=CC=C3)NC(NC4=CC=C(C=C4)C(F)(F)F)=O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    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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Product Name:
COX-2/sEH-IN-1
Cat. No.:
HY-146704
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