AZ13581837
AZ13581837 is an orally active GPR120 agonist with an EC50 of 5.2 nM for human GPR120. AZ13581837 signals through Gαq, Gαs, and β-arrestin pathways, reduces cAMP production, stimulates GLP-1 secretion, induces glucose lowering, and increases insulin secretion. AZ13581837 can be used for the research of type 2 diabetes.
For research use only. We do not sell to patients.
- CAS No.: 2896777-27-6
- Formula: C20H14N2O3S
- Molecular Weight:362.40
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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
- Purity & Documentation
- References
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Biological Activity
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GLP-1 |
AZ13581837 (1×10−9-1×10−4 M) potently activates mouse GPR120 in CHO-mGPR120 cells, inducing a DMR response with an EC50 of 4.3 nM[1].
AZ13581837 (1×10−9-1×10−4 M) induces a Gαq-dependent calcium mobilization response in CHO-hGPR120 cells with an EC50 of 120 nM[1].
AZ13581837 (1×10-9-1×10-4 M; 45 min) stimulates cAMP production in CHO-hGPR120 cells via Gαs signaling, with an EC50 of 60 nM[1].
AZ13581837 (1×10−9-1×10−4 M; 5 h) potently induces β-arrestin recruitment in U2OS-hGPR120 cells, with an EC50 of 5.2 nM[1].
AZ13581837 (10 μM; 30 min) specifically inhibits cAMP production in primary wild-type mouse islet cells, with no effect observed in GPR120 null islet cells[1].
AZ13581837 (10 μM; 2 h) induces significant GPR120-dependent secretion of active GLP-1 from STC-1 enteroendocrine cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:STC-1 mouse enteroendocrine cells
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Concentration:10 μM
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Incubation Time:2 h
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Result:Significantly increased active GLP-1 secretion from STC-1 cells compared to vehicle control, with secreted active GLP-1 levels.
AZ13581837 (35 mg/kg; p.o.; single dose 30 minutes prior to glucose bolus) enhances glucose-stimulated insulin secretion and improves glucose elimination in lean female mice via a GLP-1-dependent mechanism[1].
AZ13581837 (35 mg/kg; p.o.; single dose 30 minutes prior to glucose bolus) has glucose-lowering and insulin-stimulating effects dependent on functional GPR120, as no effects are observed in GPR120 null mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (8-week-old male, 27-32 g)[1]
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Dosage:7 mg/kg; 18 mg/kg
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Administration:p.o.; single dose 30 minutes prior to glucose load
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Result:Caused a concentration-dependent reduction in glucose excursions compared to vehicle-treated mice.
Resulted in significantly improved glucose tolerance at 18 mg/kg dose.
Achieved an unbound effective concentration (Ce50) of 0.02 μM, corresponding to exposure levels 1-3 times the in vitro EC50 for mouse GPR120 in the DMR assay.
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Animal Model:C57BL/6JOlaHSd mice (8-week-old female, 20-25 g)[1]
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Dosage:35 mg/kg
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Administration:p.o.; single dose 30 minutes prior to glucose bolus
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Result:Caused a slight but significant reduction in basal blood glucose (7.1 mM.
Significantly elevated insulin levels up to 10 minutes post glucose bolus.
Increased the acute insulin response (AIR) to ~2.4 ng/mL.
Significantly reduced plasma glucose at 20 minutes post glucose bolus.
Increased glucose elimination to ~3.8%/min.
Induced a significant increase in total GLP-1 levels compared to vehicle-treated mice.
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Animal Model:C57BL/6 wild-type mice (female, 22.5-23.0 g); C57BL/6 GPR120 null (female, 22.5 ± 0.7 g)[1]
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Dosage:35 mg/kg
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Administration:p.o.; single dose 30 minutes prior to glucose bolus
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Result:Significantly increased the acute insulin response compared to vehicle controls and increased glucose elimination in wild-type mice.
Chemical Information
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CAS No. 2896777-27-6
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Molecular Weight 362.40
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Formula C20H14N2O3S
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SMILES
O=S1(=O)C=2C=CC=CC2CN1C=3C=C(C#C)C=C(OC=4C=NC=CC4)C3
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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)
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