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Tebufelone

Catalog No. T68155   CAS 112018-00-5

Tebufelone is a potent in vitro inhibitor of CO , a novel non-steroidal anti-inflammatory drug (NSAID) belonging to the di-tert-butylphenol (DTBP) class that has shown potent anti-inflammatory, analgesic and anti-reticulitis properties in various animal models. Tebufelone potently inhibits the formation of prostaglandins (PGE2) and blocks the formation of lipoxygenase pathway products [leukotriene (LTB4)] in rat macrophages (IC50 = 20 microM) and human whole blood (IC50 = 22 microM) in vitro. = 20 microM) and human whole blood (IC50 = 22 microM) from the formation of lipoxygenase pathway products [leukotriene (LTB4)] in vitro.

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Tebufelone Chemical Structure
Tebufelone, CAS 112018-00-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 86.00
5 mg In stock $ 198.00
10 mg In stock $ 296.00
25 mg In stock $ 506.00
50 mg In stock $ 735.00
100 mg In stock $ 987.00
500 mg In stock $ 1,980.00
1 mL * 10 mM (in DMSO) In stock $ 197.00
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Purity: 99.52%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tebufelone is a potent in vitro inhibitor of CO , a novel non-steroidal anti-inflammatory drug (NSAID) belonging to the di-tert-butylphenol (DTBP) class that has shown potent anti-inflammatory, analgesic and anti-reticulitis properties in various animal models. Tebufelone potently inhibits the formation of prostaglandins (PGE2) and blocks the formation of lipoxygenase pathway products [leukotriene (LTB4)] in rat macrophages (IC50 = 20 microM) and human whole blood (IC50 = 22 microM) in vitro. = 20 microM) and human whole blood (IC50 = 22 microM) from the formation of lipoxygenase pathway products [leukotriene (LTB4)] in vitro.
In vivo Tebufelone (25, 50, 100, or 200 mg) waiting thirty minutes later, E. coli endotoxin (2 ng/kg) was administered intravenously. Oral temperatures were recorded at 15 minute intervals from 30 minutes post dosing to 8 hours post endotoxin administration. Areas under the temperature curves (AUCs), adjusted for baseline, were significantly lower than placebo for ASA and all but the 25 mg Tebufelone groups.[1]
Molecular Weight 300.44
Formula C20H28O2
CAS No. 112018-00-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (99.85 mM)

TargetMolReferences and Literature

1. Powell JH, et al. Antipyretic activity of tebufelone (NE-11740) in man. Agents Actions Suppl. 1991 ; 32:45-49. 2. Doyle MJ, et al. Comparison of tebufelone distribution in rat blood plasma and inflamed and noninflamed tissues following peroral and intravenous administration. J Pharm Sci. 1993 ; 82(8):847-850. 3. Smith BJ, et al. Characterization of the effects of tebufelone on hepatic cytochromes P450 in the beagle dog. Drug Metab Dispos. 1996 ; 24(5):523-528. 4. Sietsema WK, et al. Absorption, bioavailability, and pharmacokinetics of tebufelone in the rat. J Pharm Sci. 1993 ; 82(6):610-612. 5. Kaffenberger RM, et al. Determination of tebufelone (a new anti-inflammatory drug) strength and stability in bulk drug, dosage formulations and feed admixtures by reversed-phase high-performance liquid chromatography. J Chromatogr. 1990 ; 505(2):349-356.

Related compound libraries

This product is contained In the following compound libraries:
Membrane Protein-targeted Compound Library Inhibitor Library GPCR Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Related compounds with same targets
Aligeron Epimagnolin B Oxysophocarpine mPGES1-IN-3 ONO-8713 Darbufelone Ginsenoside Ro Schizandriside

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Keywords

Tebufelone 112018-00-5 GPCR/G Protein Immunology/Inflammation LTR Prostaglandin Receptor inhibitor inhibit

 

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