1. Metabolic Enzyme/Protease
  2. Lipoxygenase
  3. 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.

KC-11404

KC-11404 Chemical Structure

CAS No. : 148490-22-6

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Description

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[1].

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.

In Vivo

KC-11404 (oral administration; single dose) exhibits potent in vivo antihistamine activity in rats, with an ED50 of 2.8 μmol/kg[1].
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.
Molecular Weight

446.63

Formula

C28H38N4O

CAS No.
SMILES

OC1=CC2=C3C(CCC(CCCC)N3C(C)=C2CCN4CCN(CC4)C5=NC=CC(C)=C5)=C1

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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.

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KC-11404
Cat. No.:
HY-182557
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