Description
IC50: 0.03 and 0.36 μM for COX-2 and COX-1, respectively Inotilone is a cyclooxygenase (COX) inhibitor. Many of nonsteroidal anti-inflammatory drugs (NSAIDs) target cyclooxygenases (COX), which catalyze the first two steps in the biosynthesis of the prostaglandins from the substrate arachidonic acid. In vitro: Inotilone was tested as the inhibitor of mitogen-activated protein kinase, nuclear factor-κB (NF-κB), and matrix-metalloproteinase (MMP)-9 protein expressions in LPS-stimulated RAW264.7 cells. When RAW264.7 macrophages were treated with inotilone with LPS, a significant concentration-dependent inhibition of NO production was detected. It was also found that inotilone could block the protein expression of iNOS, NF-κB, and MMP-9 in LPS-stimulated RAW264.7 macrophages . In vivo: In in vivo tests, inotilone decreased the paw edema after Carr administration, and it increased the activities of catalase (CAT), superoxide dismutase (SOD), and glutathione peroxidase (GPx). Inotilone also significantly attenuated the malondialdehyde (MDA) level in the edema paw. Inotilone decreased the NO and tumor necrosis factor (TNF-α) levels on serum after Carr injection. In addition, an intraperitoneal injection treatment with inotilone could diminish neutrophil infiltration into sites of inflammation, as did indomethacin . Clinical trial: So far, no clinical study has been conducted.
Product information
CAS Number: 906366-79-8
Molecular Weight: 218.21
Formula: C12H10O4
Chemical Name: (2Z)-2-[(3,4-dihydroxyphenyl)methylidene]-5-methyl-2,3-dihydrofuran-3-one
Smiles: CC1=CC(=O)/C(=C/C2C=C(O)C(O)=CC=2)/O1
InChiKey: NLZQGBCUKNUDED-SDQBBNPISA-N
InChi: InChI=1S/C12H10O4/c1-7-4-11(15)12(16-7)6-8-2-3-9(13)10(14)5-8/h2-6,13-14H,1H3/b12-6-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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