1. Immunology/Inflammation Metabolic Enzyme/Protease
  2. COX Phospholipase
  3. VI-60

VI-60 is a dual, orally active inhibitor of cPLA2 and COX-2, which reveals an anti-inflammtory efficacy through the inhibition of p38 MAPK/cPLA2/COX-2/PGE2 pathway.

For research use only. We do not sell to patients.

VI-60 Chemical Structure

VI-60 Chemical Structure

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Description

VI-60 is a dual, orally active inhibitor of cPLA2 and COX-2, which reveals an anti-inflammtory efficacy through the inhibition of p38 MAPK/cPLA2/COX-2/PGE2 pathway[1].

IC50 & Target

COX-2

 

cPLA2

 

In Vitro

VI-60 (10 μΜ, 24-48 h) inhibits the LPS-induced inflammatory mediators NO (IC50 is 3.85 μM) and PGE2 production without significant cytotoxicity in RAW264.7 cells[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: RAW264.7
Concentration: 30 μΜ
Incubation Time: 24-48 h
Result: Exhibite cell viability of nearly 100%, in compare to the verhicle group.

Western Blot Analysis[1]

Cell Line: RAW264.7
Concentration: 30 μΜ, 2.5-10 μM
Incubation Time: 30 μM for 2 h, 2.5-10 μM for 1 h
Result: Downregulated the phosphor-p38-MAPK, cPLA2 and COX2, stabilized the cPLA2 and COX2 proteins when heated.
In Vivo

VI-60 (20 mg/kg, p.o., everyday or every two days) ameliorates the adjuvant-induced arthritis, exhibits analgesic activity in Lewis rats[1].
VI-60 (20 mg/kg, p.o., everyday) regulates the balance between Th17 and Tregs and reduces IL-17 expression through inhibition of the p38 MAPK/cPLA2/COX-2/PGE2 pathway[1].
VI-60 exhibits a low ulcerative potential (50 mg/kg), no hepatotoxicity or nephrotoxicity (20 mg/kg, p.o.) in Wistar rats .

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

Animal Model: Adjuvant-induced arthritis in Lewis rats[1]
Dosage: 20 mg/kg
Administration: p.o., every 24 h or 48 h for 20 days
Result: Inhibited the weight loss and the edema of paws, increased the mechanical withdrawal threshold (MWT), decreased the spleen weights.
Animal Model: Male mistar rats[1]
Dosage: 20 mg/kg
Administration: p.o., for 3 days
Result: Revealed identical indexes of glutamic pyruvic transaminase (GPT), glutamic oxalacetic transaminase (GOT), and blood urea nitrogen (BUN) as of normal rats.
Molecular Weight

592.73

Formula

C37H43F3O3

SMILES

CCCCC/C=C\C/C=C\C/C=C\C/C=C\CC/C=C(C(F)(F)F)/OC(C(C)C1=CC=C(C(C2=CC=CC=C2)=O)C=C1)=O

Shipping

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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Help & FAQs
  • 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:
VI-60
Cat. No.:
HY-162228
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