GPR4 antagonist 2
GPR4 antagonist 2 is a selective GPR4 antagonist with an IC50 of 67 nM. GPR4 antagonist 2 inhibits pH-dependent GPR4 activation and CRE-driven transcriptional activity. GPR4 antagonist 2 prolongs the survival of mice in a myocardial infarction model. GPR4 antagonist 2 can be used for research on myocardial infarction.
For research use only. We do not sell to patients.
- CAS No.: 1883333-94-5
- Formula: C31H37N5
- Molecular Weight:479.67
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 3b
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Antagonist activity at N-terminal HA-tagged OGR1 (unknown origin) expressed in HEK293 cells assessed as inhibition of pH dependent nuclear factor of activated T-cell activity at pH 7.2 incubated for 6 hrs by dual luciferase reporter gene assay
Antagonist activity at N-terminal HA-tagged OGR1 (unknown origin) expressed in HEK293 cells assessed as inhibition of pH dependent nuclear factor of activated T-cell activity at pH 7.2 incubated for 6 hrs by dual luciferase reporter gene assay
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[PMID: 27190599] |
| HEK293 | IC50 |
67 nM
Compound: 3b
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Antagonist activity at N-terminal HA-tagged GPR4 (unknown origin) expressed in HEK293 cells assessed as inhibition of pH dependent cAMP response element-driven transcriptional activity at pH 7.2 incubated for 6 hrs by dual luciferase reporter gene assay
Antagonist activity at N-terminal HA-tagged GPR4 (unknown origin) expressed in HEK293 cells assessed as inhibition of pH dependent cAMP response element-driven transcriptional activity at pH 7.2 incubated for 6 hrs by dual luciferase reporter gene assay
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[PMID: 27190599] |
In Vitro
GPR4 antagonist 2 (10 μM) shows no activity against TDAG8 or OGR1 in HEK293 cells expressing these receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice were subjected to permanent left anterior descending coronary artery ligation under anesthetized conditions[1]
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Dosage:6.7 mg/kg/day
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Administration:i.p.; twice a day; from 1 day before to 7 days after the operation
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Result:Achieved 100% survival (7/7) in mice with myocardial infarction, compared to 1/7 survival in controls.
Chemical Information
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CAS No. 1883333-94-5
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Molecular Weight 479.67
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Formula C31H37N5
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SMILES
N=1C(=CC(=C2N=C(N(C12)CC3=CC=C4NC5=CC=C(C=C5CCC4=C3)CN6CCCCC6)CC)C)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)
GPR4 antagonist 2 Related Classifications
HY-101537 Related Classifications
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