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.
For research use only. We do not sell to patients.
- CAS No.: 134822-78-9
- Formula: C17H16N2O4
- Molecular Weight:312.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
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 No. 134822-78-9
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Molecular Weight 312.32
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CGS 23885 Related Classifications
HY-182422 Related Classifications
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