2. Metabolic Enzyme/Protease GPCR/G Protein
  3. Lipoxygenase Leukotriene Receptor
  4. 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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CGS 23885

CGS 23885 Chemical Structure

CAS No. : 134822-78-9

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CGS 23885 Related Antibodies

Top Publications Citing Use of Products

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5-LOX 12-LOX 15-LOX

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LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

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Description

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[1][2].

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.

CGS 23885 Related Antibodies
In Vivo

CGS 23885 (1-30 mg/kg; p.o.; administered 1 h prior to carrageenan injection and 1 h prior to A23187 injection) dose-dependently inhibits A23187 (HY-N6687)-induced biosynthesis of LTB4 and LTC4/D4/E4 in a rat pleurisy model, and the drug concentration in pleural effusion shows a strong positive correlation with the inhibitory effect on LTB4 (IC50 = 21 ng/mL)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (male, 220-235 g, pleurisy induced by intrapleural κ-carrageenan and calcium ionophore A23187)[2]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; 1 h before carrageenan injection and 1 h before A23187 injection
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.
Molecular Weight

312.32

Formula

C17H16N2O4
CAS No.
SMILES

O=C(N(CC1=CC2=C(OC1)C=CC(OC3=CC=CC=C3)=C2)O)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CGS 23885 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CGS 23885134822-78-9CGS23885CGS-23885LipoxygenaseLeukotriene ReceptorLOXdog5-lipoxygenaseleukotriene B4human5-hydroxyeicosatetraenoic acid12-lipoxygenasesheep cyclooxygenaseleukotriene C4/D4/E4guinea pigcarrageenan-induced rat pleurisyInhibitorinhibitorinhibit

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