GPBAR-A
GPBAR-A is a specific agonist of the bile acid receptor GPBAR1. GPBAR-A can be used for the research of diabetes mellitus.
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- No. CAS: 877052-79-4
- Fòrmula: C23H15F7N2O2
- Peso molecular:484.37
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.019 μM
Compound: 2
|
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
Agonist activity at human TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
|
[PMID: 24007860] |
| HEK293 | EC50 |
0.13 μM
Compound: 2
|
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
Agonist activity at mouse TGR5 expressed in HEK293 cells assessed CRE-induced luciferase activity after 5.5 hrs by reporter gene assay
|
[PMID: 24007860] |
| HEK293 | EC50 |
0.23 nM
Compound: 3
|
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay
Agonist activity at human TGR5 expressed in HEK293 cells incubated for 5.5 hrs by CRE-driven luciferase reporter gene assay
|
[PMID: 23148522] |
GPBAR-A (3 μM; 24-36 h) stimulates the release of glucagon-like peptide (GLP-1) in GLUTag cells[1].
GPBAR-A (3 μM; 24-36 h) increases GLP-1 release 4.2-fold in primary colonic cultures[1].
GPBAR-A (3 μM; 24-36 h) increases GLP-1 release 2.6-fold in upper small intestinal cultures[1].
GPBAR-A (3 μM; 24-36 h) also increases the cAMP concentration in GLUTag cells by 57%[1].
GPBAR-A (3 μM; 24-36 h) increases GLP-1 secretion in the presence of diazoxide (KATP channel opener, 340 μM) and 70 mM KCl[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 877052-79-4
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Peso molecular 484.37
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Fòrmula C23H15F7N2O2
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SMILES
O=C1N(CC2=C(C3=C(F)C=CC=C3)C=CN=C2OC1)CC4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)