CGS 23885
CGS 23885 is an orally active 5-lipoxygenase (5-lipoxygenase) inhibitor. CGS 23885 reduces the production of 5-hydroxyeicosatetraenoic acid (5-hydroxyeicosatetraenoic acid), LTB4, and LTC4/D4/E4. CGS 23885 inhibits cell infiltration in rat pleurisy. CGS 23885 can be used in pleurisy-related research.
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- CAS. Nr.: 134822-78-9
- Formel: C17H16N2O4
- Molecular Weight:312.32
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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
Beschreibung
IC50 & Target
[1]|
LTB4 |
5-LOX |
In Vitro
CGS 23885 (Compound 43) potently inhibits 5-lipoxygenase activity in guinea pig polymorphonuclear leukocytes (PMNs), with an IC50 value of 43 nM for the inhibition of 5-HETE production and an IC50 value of 48 nM for the inhibition of LTB4 production[1].
CGS 23885 weakly inhibits ram seminal vesicle cyclooxygenase with an IC50 of 36 μM, and exhibits high selectivity for 5-lipoxygenase[1].
CGS 23885 moderately inhibits human platelet 12-lipoxygenase with an IC50 of 0.64 μM[1].
CGS 23885 inhibits 5-lipoxygenase activity in canine whole blood with an IC50 of 0.11 μM[1].
CGS 23885 inhibits the activity of 5-lipoxygenase in human whole blood with an IC50 of 0.89 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (male, 220-235 g, pleurisy induced by intrapleural κ-carrageenan and calcium ionophore A23187)[2]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; 1 h before carrageenan injection and 1 h before A23187 injection
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Result:Inhibited A23187-enhanced LTB4 biosynthesis by 32% and LTC4/D4/E4 biosynthesis by 4% at 1 mg/kg.
Inhibited A23187-enhanced LTB4 biosynthesis by 73% and LTC4/D4/E4 biosynthesis by 33-35% at 3 mg/kg.
Inhibited A23187-enhanced LTB4 biosynthesis by 93% and LTC4/D4/E4 biosynthesis by 52-67% at 10 mg/kg.
Inhibited A23187-enhanced LTB4 biosynthesis by 97% and caused a 24% significant reduction in total cellular influx at 30 mg/kg.
Showed a positive correlation between pleural fluid concentration and inhibition of LTB4 biosynthesis, with an IC50 of 21 ng/mL for LTB4 inhibition.
Produced no significant effect on exudate volume, PGE2 levels, or TXB2 levels at all doses; no significant effect on total cellular influx at 1, 3, 10 mg/kg.
Chemical Information
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CAS. Nr. 134822-78-9
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Molecular Weight 312.32
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Formel C17H16N2O4
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SMILES
O=C(N(CC1=CC2=C(OC1)C=CC(OC3=CC=CC=C3)=C2)O)N
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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
[1]. Satoh Y, et al. Substituted chromenes as potent, orally active 5-lipoxygenase inhibitors. J Med Chem. 1993;36(23):3580-3594. [Content Brief]
[2]. Raychaudhuri A, et al. Inhibition of LTB4 biosynthesis in situ by CGS 23885, a potent 5-lipoxygenase inhibitor, correlates with its pleural fluid concentrations in an experimentally induced rat pleurisy model. Naunyn Schmiedebergs Arch Pharmacol. 1997;355(4):470-474. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CGS 23885 Related Classifications
HY-182422 Related Classifications
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