AZ-11665362
AZ-11665362 is a CRTh2 (DP2) receptor antagonist with an IC50 of 2.6 nM. AZ-11665362 shows weak activity against aldose reductase, serotonin transporter, CYP 2C19, and CYP 2C9. AZ-11665362 lacks measurable inhibitory activity against COX-1 and COX-2. AZ-11665362 can be used for the research of asthma, and other inflammatory diseases.
For research use only. We do not sell to patients.
- CAS No.: 629645-40-5
- Formula: C22H20N2O2
- Molecular Weight:344.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
DP2 2.6 nM (IC50) |
CYP2C19 2.5 μM (IC50) |
CYP2C9 5 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
2.6 nM
Compound: 12
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Displacement of [3H]PGD2 from human CRTh2 expressed in HEK293 cells
Displacement of [3H]PGD2 from human CRTh2 expressed in HEK293 cells
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[PMID: 16753296] |
In Vitro
AZ-11665362 (Compound 12) potently binds to human CRTh2 expressed in HEK 293 cells, with an IC50 of 2.6 nM[1].
AZ-11665362 shows selective activity against rat aldose reductase, serotonin transporter, CYP 2C19, and CYP 2C9 (IC50 values of 150, 2000, 2500 and 5000 μM), with no measurable activity against COX-1 or COX-2 at 3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 629645-40-5
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Molecular Weight 344.41
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Formula C22H20N2O2
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SMILES
O=C(O)CN1C=2C=CC(=CC2C(C=3C=CN=C4C3C=CC=C4C)=C1C)C
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)