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
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
2.6 nM
Compound: 12
|
Displacement of [3H]PGD2 from human CRTh2 expressed in HEK293 cells
Displacement of [3H]PGD2 from human CRTh2 expressed in HEK293 cells
|
[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.
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- AZ-11665362
- 629645-40-5
- AZ11665362
- AZ 11665362
- Prostaglandin Receptor
- Serotonin Transporter
- Aldose Reductase
- Cytochrome P450
- 5-HTT
- SERT
- SLC6A4
- AKR1B1
- Aldo-keto reductase family 1 member B
- CYPs
- HEK 293 cells
- COX-2
- serotonin transporter
- hERG channel
- rat aldose reductase
- CYP 2C9
- CRTh2 (DP2) receptor
- COX-1
- DP1 receptor
- CYP 2C19
- Inhibitor
- inhibitor
- inhibit