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.
For research use only. We do not sell to patients.
- CAS No.: 148490-22-6
- Formula: C28H38N4O
- Molecular Weight:446.63
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
5-LOX 0.9 μM (IC50) |
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.
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.
-
Animal Model:unspecified strain[1]
-
Dosage:50 μmol/kg
-
Administration:p.o.; single dose
-
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
-
CAS No. 148490-22-6
-
Molecular Weight 446.63
-
Formula C28H38N4O
-
SMILES
OC1=CC2=C3C(CCC(CCCC)N3C(C)=C2CCN4CCN(CC4)C5=NC=CC(C)=C5)=C1
-
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
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Powered by Bioz