2. GPCR/G Protein Neuronal Signaling
  3. GPR119 Arrestin GLP Receptor
  4. 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.

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AZ13581837

AZ13581837 Chemical Structure

CAS No. : 2896777-27-6

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AZ13581837 Related Antibodies

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Description

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[1].

IC50 & Target[1]

GLP-1

 

In Vitro

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.

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[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 mice (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 mice (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 mice (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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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-13581837GPR119ArrestinGLP ReceptorG Protein-Coupled Receptor 119GαqCHO-mGPR120 cellstype 2 diabetesCHO-hGPR120 cellsGPR120GLP-1GαsSTC-1 enteroendocrine cellscAMPβ-arrestinInhibitorinhibitorinhibit

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