GPR81 agonist 2
GPR81 agonist 2 is a GPR81 agonist with an EC50 of 0.023 μM for the human receptor. GPR81 agonist 2 activates the lactate-sensing receptor GPR81, inhibits forskolin-stimulated cAMP production and GTP binding of Gi protein. GPR81 agonist 2 can be used for research on type 2 diabetes.
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- CAS No.: 1143024-28-5
- Formule: C26H27ClN6O5S2
- Masse moléculaire:603.11
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
GPR81 0.023 μM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.023 μM
|
Agonist activity against human GPR81 overexpressing CHO cells assessed by functional cell-based cAMP assay.
Agonist activity against human GPR81 overexpressing CHO cells assessed by functional cell-based cAMP assay.
|
31932225 |
In Vitro
GPR81 agonist 2 (compound 1) (10 μM) acts as a potent GPR81 agonist in CHO cells overexpressing hGPR81[1].
GPR81 agonist 2 has hGPR81 EC50 = 0.023 µM, hGPR109A EC50 = 0.123 µM, and hGHS-R1a IC50 = 0.008 µM; it shows poor selectivity for hGPR109A and hGHS-R1a[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. 1143024-28-5
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Masse moléculaire 603.11
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Formule C26H27ClN6O5S2
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SMILES
O=C(NC1=NC2=C(S1)C=C(S(=O)(C3CCN(CC3)C)=O)C=C2)NC(C4=C(Cl)C=C(OCC)C(N5N=CC=C5)=C4)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)