2. GPCR/G Protein Neuronal Signaling
  3. GPR119
  4. AZ13581837

AZ13581837 is a GPR120 agonist with oral effectiveness, human EC50 values of 5.2 nM, and mouse EC50 of 4.3 nM. 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.

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AZ13581837

AZ13581837 Chemical Structure

CAS No. : 2896777-27-6

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Description

AZ13581837 is a GPR120 agonist with oral effectiveness, human EC50 values of 5.2 nM, and mouse EC50 of 4.3 nM. 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[1].

In Vitro

AZ13581837 (1×10−9 to 1×10−4 M) potently activates human GPR120 in CHO-hGPR120 cells, inducing a GPR120-specific DMR response with an EC50 of 5.2 nM[1].
AZ13581837 (1×10−9 to 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 to 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 to 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 to 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.

AZ13581837 Related Antibodies

ELISA Assay[1]

Cell Line: STC-1 mouse enteroendocrine cells
Concentration: 10 μM
Incubation Time: 2 h
Result: Significantly increased active GLP-1 secretion from STC-1 cells compared to vehicle control, with secreted active GLP-1 levels.
In Vivo

AZ13581837 (7-18 mg/kg; p.o.; single dose 30 minutes prior to glucose load) improves oral glucose tolerance in lean male mice with a CE50 of 0.02 μM, with significant effects observed at 18 mg/kg[1].
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.

Animal Model: C57BL/6 (8-week-old male, 27-32 g)[1]
Dosage: 7 mg/kg; 18 mg/kg
Administration: p.o.; single dose 30 minutes prior to glucose load
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.
Animal Model: C57BL/6JOlaHSd (8-week-old female, 20-25 g)[1]
Dosage: 35 mg/kg
Administration: p.o.; single dose 30 minutes prior to glucose bolus
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.
Animal Model: C57BL/6 wild-type (female, 22.5-23.0 g); C57BL/6 GPR120 null (female, 22.5 ± 0.7 g)[1]
Dosage: 35 mg/kg
Administration: p.o.; single dose 30 minutes prior to glucose bolus
Result: Significantly increased the acute insulin response compared to vehicle controls and increased glucose elimination in wild-type mice.
Molecular Weight

362.40

Formula

C20H14N2O3S
CAS No.
SMILES

O=S1(=O)C=2C=CC=CC2CN1C=3C=C(C#C)C=C(OC=4C=NC=CC4)C3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AZ13581837 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZ135818372896777-27-6AZ 13581837AZ-13581837GPR119G Protein-Coupled Receptor 119GαqCHO-mGPR120 cellstype 2 diabetesCHO-hGPR120 cellsGPR120GLP-1GαsSTC-1 enteroendocrine cellscAMPβ-arrestinInhibitorinhibitorinhibit

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