A dual CysLT1 receptor and TP receptor antagonist
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KP496

Item No. 46561

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[[4-[[(4-chlorophenyl)sulfonyl]amino]butyl][[3-[[4-(1-methylethyl)-2-thiazolyl]methoxy]phenyl]methyl]amino]sulfonyl]-benzoic acid
CAS Number
217799-03-6
Molecular Formula
C31H34ClN3O7S3
Formula Weight
692.3
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
ClC1=CC=C(S(=O)(NCCCCN(S(=O)(C2=C(C(O)=O)C=CC=C2)=O)CC3=CC(OCC4=NC(C(C)C)=CS4)=CC=C3)=O)C=C1
InChi Code
InChI=1S/C31H34ClN3O7S3/c1-22(2)28-21-43-30(34-28)20-42-25-9-7-8-23(18-25)19-35(45(40,41)29-11-4-3-10-27(29)31(36)37)17-6-5-16-33-44(38,39)26-14-12-24(32)13-15-26/h3-4,7-15,18,21-22,33H,5-6,16-17,19-20H2,1-2H3,(H,36,37)
InChi Key
WMMCMKVGDPXYQS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $219

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    5 mg

    $548

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    10 mg

    $876

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    25 mg

    $1,643

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    Product Description

    KP496 is a dual antagonist of the cysteinyl leukotriene 1 (CysLT1) receptor and TP receptor.1 It inhibits contractions induced by leukotriene D4 (LTD4; Item No. 20310) or U-46619 (Item No. 16450) in guinea pig tracheal segments (pA2s = 8.64 and 8.23, respectively) but not those induced by histamine, acetylcholine (ACh), serotonin (5-HT), or substance P at 10 µM, and it does not affect β2-adrenergic receptor (β2-AR) agonist-induced relaxation in precontracted guinea pig tracheal segments at 10 µM. However, KP496 does inhibit contractions induced by prostaglandin D2 (PGD2) or PGF2α in guinea pig tracheal segments at 0.1 and 1 µM, respectively. Intranasal administration of KP496 (0.05%) decreases cedar pollen-induced increases in specific airway resistance in a guinea pig model of allergic rhinitis.2 It decreases fibrosis, inflammation, and bronchoalveolar lavage fluid (BALF) immune cell infiltration in a mouse model of pulmonary fibrosis induced by bleomycin (Item No. 13877).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ishimura, M., Kataoka, S., Suda, M., et al. Effects of KP-496, a novel dual antagonist for leukotriene D4 and thromboxane A2 receptors, on contractions induced by various agonists in the guinea pig trachea. Allergol. Int. 55(4), 403-410 (2006).

    2. Mizutani, N., Suda, M., Ishimura, M., et al. Effects of KP-496, a novel dual antagonist of leukotriene D4 and thromboxane A2 receptors on nasal blockage in guinea pig models of allergic rhinitis. Inflamm. Res. 57(6), 247-251 (2008).

    3. Kurokawa, S., Suda, M., Okuda, T., et al. Effect of inhaled KP-496, a novel dual antagonist of the cysteinyl leukotriene and thromboxane A2 receptors, on a bleomycin-induced pulmonary fibrosis model in mice. Pulm. Pharmacol. Ther. 23(5), 425-431 (2010).