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.
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- CAS. Nr.: 3050874-42-2
- Formel: C37H43F3O3
- Molecular Weight:592.73
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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COX-2 |
cPLA2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
3.85 μM
Compound: VI-60
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Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of NO production pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by griess reagent based assay
Antiinflammatory activity in LPS-induced mouse RAW264.7 cells assessed as inhibition of NO production pretreated for 1 hr followed by LPS stimulation and measured after 24 hrs by griess reagent based assay
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[PMID: 38286094] |
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.
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Cell Line:RAW264.7
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Concentration:30 μΜ
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Incubation Time:24-48 h
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Result:Exhibite cell viability of nearly 100%, in compare to the verhicle group.
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Cell Line:RAW264.7
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Concentration:30 μΜ, 2.5-10 μM
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Incubation Time:30 μM for 2 h, 2.5-10 μM for 1 h
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Result:Downregulated the phosphor-p38-MAPK, cPLA2 and COX2, stabilized the cPLA2 and COX2 proteins when heated.
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.
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Animal Model:Adjuvant-induced arthritis in Lewis rats[1]
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Dosage:20 mg/kg
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Administration:p.o., every 24 h or 48 h for 20 days
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Result:Inhibited the weight loss and the edema of paws, increased the mechanical withdrawal threshold (MWT), decreased the spleen weights.
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Animal Model:Male mistar rats[1]
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Dosage:20 mg/kg
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Administration:p.o., for 3 days
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Result:Revealed identical indexes of glutamic pyruvic transaminase (GPT), glutamic oxalacetic transaminase (GOT), and blood urea nitrogen (BUN) as of normal rats.
Chemical Information
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CAS. Nr. 3050874-42-2
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Molecular Weight 592.73
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Formel C37H43F3O3
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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