CGS 22745
CGS 22745 is a selective and orally active 5-Lipoxygenase inhibitor. CGS 22745 blocks the conversion of Arachidonic acid (HY-109590) to 5-HETE (HY-113434B) and leukotrienes. CGS 22745 inhibits A23187-stimulated LTB4 (HY-107608) formation in whole blood. CGS 22745 inhibits exudate formation and PMN accumulation in Carrageenan (HY-125474)-induced pleurisy. CGS 22745 can be used for research on inflammatory diseases.
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- CAS. Nr.: 131817-86-2
- Formel: C16H18N2O2
- Molecular Weight:270.33
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
5-LOX |
In Vitro
CGS 22745 does not appreciably inhibit the cell-free enzymes cyclooxygenase from ram seminal vesicles, thromboxane synthase and 12-lipoxygenase from human platelets, or 15-lipoxygenase from human neutrophils[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 (Elimination) |
|---|---|---|---|
| Dog[1] | 1 mg/kg | i.v. | >160 min |
In Vivo
CGS 22745 (3-30 mg/kg; p.o.) demonstrates dose-dependent in vivo anti-inflammatory activity in the rat Carrageenan (HY-125474)-induced pleurisy model, reducing exudate volume, mononuclear cells, and PMNs during the late phase (48 and 72 hr)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beagle dogs (male or female, Barton Farms, 8-15 kg)[1]
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Dosage:1 mg/kg (i.v.); 0.3, 3, 10 mg/kg (p.o.)
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Administration:i.v.; bolus (1 mg/kg); p.o.; by intubation (0.3, 3, 10 mg/kg)
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Result:Inhibited A23187-stimulated LTB4 formation by 96% at 5 min with an effective biological half-life of >160 min following 1 mg/kg i.v.
Inhibited A23187-induced LTB4 formation dose-dependently at 1 hr: 46% at 0.3 mg/kg (duration of action 0.9 hr), 90% at 3 mg/kg (duration of action 3.0 hr), and 98% at 10 mg/kg (duration of action 6.0 hr) after oral dosing.
Exhibited ED50 values of 0.39, 3.0, and 19.2 mg/kg at 1, 3, and 6 hr after oral dosing, respectively.
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Animal Model:Sprague Dawley rats (male, Charles River)[1]
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Dosage:3, 10, 30 mg/kg
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Administration:p.o.
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Result:Reduced exudate volume by 32%, mononuclear cells by 21%, and PMNs by 24% at 48 hr at 10 mg/kg p.o.
Reduced exudate volume by 42%, mononuclear cells by 36%, and PMNs by 64% at 72 hr at 10 mg/kg p.o.
Dose-dependently inhibited exudate formation, mononuclear cell influx, and PMN accumulation during the late phase (48 and 72 hr).
Chemical Information
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CAS. Nr. 131817-86-2
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Molecular Weight 270.33
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Formel C16H18N2O2
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SMILES
CC=1N(C2=CC=C(/C=C/C(N(C)O)=O)C=C2)C(C)=CC1
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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
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
CGS 22745 Related Classifications
HY-187594 Related Classifications
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