CP-288886
CP-288886 is a cysLT1 receptor antagonist with a Ki value of 0.004 μM. CP-288886 exhibits comparable activity to Zafirlukast (HY-17492) and Pranlukast (HY-B0290). CP-288886 inhibits calcium mobilization with an IC50 of 0.0005 μM in human U937 cells. CP-288886 has high oral bioavailability. CP-288886 possesses anti-asthmatic activity in a guinea pig asthma model and can be used for the research of diseases such as asthma.
For research use only. We do not sell to patients.
- CAS No.: 221332-74-7
- Formula: C30H28ClF3N2O6S
- Molecular Weight:637.07
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
CysLT1 0.004 μM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-937 | IC50 |
0.0005 μM
Compound: 7
|
Compound was tested for its ability to inhibit calcium influx in human U937 cells
Compound was tested for its ability to inhibit calcium influx in human U937 cells
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[PMID: 9934474] |
Chemical Information
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CAS No. 221332-74-7
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Molecular Weight 637.07
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Formula C30H28ClF3N2O6S
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SMILES
O[C@H]1C2=CC(OCC3=NC4=CC(Cl)=CC=C4C=C3)=CC=C2OC(C)(C)[C@H]1CC5=C(C=CC(NS(C(F)(F)F)(=O)=O)=C5)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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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.
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Ovalbumin-Induced Allergic Airway Inflammation
Ovalbumin-induced allergic airway inflammation is a mouse model in which systemic sensitization to ovalbumin, usually with aluminum hydroxide adjuvant, is followed by airway ovalbumin challenge to induce allergic airway inflammation, eosinophil recruitment, mucus production, serum antigen-specific IgE, Th2 cytokine responses, and airway hyperresponsiveness to methacholine. The model is used to study allergen-driven airway inflammation and asthma-like immune responses, but it does not reproduce every feature of human asthma. The main readouts are bronchoalveolar lavage fluid cellularity, lung histopathology, airway hyperresponsiveness, serum OVA-specific IgE, and cytokines such as IL-4, IL-5, and IL-13 in bronchoalveolar lavage fluid or lung samples. Eosinophilia and Th2 cytokines reflect allergic type 2 inflammation, while methacholine responsiveness provides a functional airway-reactivity endpoint.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)