Cefetecol hydrate
Cefetecol hydrate (GR69153 hydrate) is a semisynthetic β-lactam antibacterial agent and α-glucosidase inhibitor (yeast IC50 = 2.1 μM; Ki = 5.78 μM) that crosses the blood-brain barrier. Cefetecol hydrate reduces blood glucose levels in Streptozotocin-induced diabetic mice. Cefetecol hydrate decreases the mRNA expression of GSK-3, PPAR-γ, and UCP-3. Cefetecol hydrate induces bacterial cell filamentation and exhibits bactericidal activity against Gram-positive and Gram-negative bacteria. Cefetecol hydrate is used in the study of diabetes and bacterial infections.
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- CAS No.: 127182-67-6
- Formule: C20H25N5O13S2
- Masse moléculaire:607.57
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vivo
Cefetecol (subcutaneous injection; twice) hydrate effectively inhibits the formation of experimental subcutaneous abscesses caused by S. aureus in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6NKist (female, streptozotocin-induced diabetic model)[1]
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Dosage:30 mg/kg/day
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Administration:i.p.; daily; 14 days
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Result:Decreased blood glucose levels by as much as 30% (195.3 mg/dl) compared to control animals.
Slightly decreased mRNA expression levels of GSK-3, PPAR-γ and UCP-3 compared to the internal control GAPDH.
Did not significantly change the expression levels of aldose reductase and PTP-1B.
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Animal Model:ddY (male, 22~25 g, 7 mice/group)[3]
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Dosage:0.10-0.95 mg/mouse (single); 0.02-0.31 mg/mouse (three doses)
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Administration:s.c.; once (1 hour after challenge) or three times (1-hour intervals starting 1 hour after challenge); 7~10 days
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Result:Produced ED50 values of 0.17, 0.21, 0.10, 0.12, 0.36, 0.12, 0.28, 0.10, 0.22, 0.35, and 0.95 mg/mouse against S. pyogenes J-12, S. pyogenes J-13, S. pneumoniae TO-1, E. coli 11, E. coli 49, E. coli 54, K. pneumoniae 3K25, K. pneumoniae 15C, P. mirabilis 9', P. mirabilis 1287, and P. mirabilis JU-453, respectively, with single administration.
Produced ED50 values of 0.02, 0.07, 0.13, 0.18, 0.20, and 0.31 mg/mouse against S. pneumoniae TO-1, E. coli 11, E. coli 49, K. pneumoniae 3K25, P. mirabilis 9', and P. mirabilis JU-453, respectively, with three doses.
Exhibited good efficacy against P. mirabilis JU-453 (MIC of 200 μg/mL).
Chemical Information
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CAS No. 127182-67-6
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Masse moléculaire 607.57
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Formule C20H25N5O13S2
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SMILES
O=C1N2[C@@](SCC=C2C(O)=O)([H])[C@@H]1NC(/C(C3=CSC(N)=N3)=N\O[C@@H](C4=CC(O)=C(C=C4)O)C(O)=O)=O.O.O.O.O
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Synonyms
GR69153 hydrate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Lee DS, et al. Ceftezole, a cephem antibiotic, is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity. International journal of molecular medicine. 2007 Sep;20(3):379-83. [Content Brief]
[2]. Harada Y, et al. Ceftezole, a new cephalosporin C derivative II. Distribution and excretion in parenteral administration. J Antibiot (Tokyo). 1976 Oct;29(10):1071-82. [Content Brief]
[3]. Noto T, et al. Ceftezole, a new cephalosporin C derivative I. In vitro and in vivo antimicrobial activity. The Journal of antibiotics. 1976 Oct;29(10):1058-70. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cefetecol hydrate Related Classifications
HY-159796 Related Classifications
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Keywords
- Cefetecol
- 127182-67-6
- GR69153
- GR 69153
- GR-69153
- Glycosidase
- Bacterial
- GSK-3
- PPAR
- Glycogen synthase kinase-3
- Glycogen synthase kinase 3
- Peroxisome proliferator-activated receptors
- UCP-3
- S. aureus
- α-glucosidase inhibitor
- gram-negative
- gram-positive
- streptozotocin-induced diabetic mice
- blood-brain barrier
- S. pyogenes
- PPAR-γ
- Inhibitor
- inhibitor
- inhibit