KC-11404
KC-11404 is an orally active antihistamine and 5-lipoxygenase inhibitor, with an IC50 of 0.9 μM against guinea pig 5-lipoxygenase. KC-11404 inhibits histamine-induced contraction of isolated guinea pig ileum with an IC50 of 0.26 μM. KC-11404 inhibits PAF-induced rabbit platelet aggregation with an IC50 of 2.0 μM. It inhibits the histamine phase of antigen-induced bronchoconstriction and PAF-induced bronchoconstriction in guinea pigs. KC-11404 can be used for the research of asthma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 148490-22-6
- Formel: C28H38N4O
- Molecular Weight:446.63
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
5-LOX 0.9 μM (IC50) |
In Vitro
KC-11404 potently inhibits histamine-induced contractions of isolated guinea pig ileum with an IC50 of 0.26 μM[1].
KC-11404 inhibits PAF-induced aggregation of rabbit platelets with an IC50 of 2.0 μM[1].
KC-11404 (10 μM) completely inhibits semipurified guinea pig PMN 5-lipoxygenase with an IC50 of 0.9 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
KC-11404 (oral administration; single dose) potently inhibits passive cutaneous anaphylaxis in rats, with an ED50 of 0.9 μmol/kg[1].
KC-11404 (oral administration; single dose) inhibits the histamine phase of antigen-induced bronchoconstriction in guinea pigs, with an ED50 of 1.9 μmol/kg[1].
KC-11404 (oral administration; single dose) inhibits PAF-induced bronchoconstriction in guinea pigs, with an ED50 of 2.1 μmol/kg[1].
KC-11404 (50 μmol/kg; p.o.; single administration) exhibits efficacy comparable to that of Zileuton (HY-14164) in inhibiting the leukotriene-dependent phase of antigen-induced bronchoconstriction in guinea pigs at a dose of 50 μmol/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:unspecified strain[1]
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Dosage:50 μmol/kg
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Administration:p.o.; single dose
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Result:Inhibited changes in airway resistance by 53% (5 hours pre-challenge) and 53% (8 hours pre-challenge).
Inhibited changes in dynamic compliance by 31% (5 hours pre-challenge) and 37% (8 hours pre-challenge).
Showed equivalent potency to zileuton, with no significant difference between the two compounds at either time point.
Chemical Information
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CAS. Nr. 148490-22-6
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Molecular Weight 446.63
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Formel C28H38N4O
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SMILES
OC1=CC2=C3C(CCC(CCCC)N3C(C)=C2CCN4CCN(CC4)C5=NC=CC(C)=C5)=C1
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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.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
[1]. Paris D, et al. Synthesis, structure-activity relationships, and pharmacological evaluation of pyrrolo[3,2,1-ij]quinoline derivatives: potent histamine and platelet activating factor antagonism and 5-lipoxygenase inhibitory properties. Potential therapeutic application in asthma. J Med Chem. 1995;38(4):669-685. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
KC-11404 Related Classifications
HY-182557 Related Classifications
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