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 No.: 131817-86-2
- 화학식: C16H18N2O2
- 분자량:270.33
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
5-LOX |
In Vitro
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
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 No. 131817-86-2
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분자량 270.33
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CGS 22745 Related Classifications
HY-187594 Related Classifications
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