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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 2896777-27-6
- Formule: C20H14N2O3S
- Masse moléculaire:362.40
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Protocole
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform Arrestin
More
Activité biologique
Description
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.
-
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 (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.
Chemical Information
-
CAS No. 2896777-27-6
-
Masse moléculaire 362.40
-
Formule C20H14N2O3S
-
SMILES
O=S1(=O)C=2C=CC=CC2CN1C=3C=C(C#C)C=C(OC=4C=NC=CC4)C3
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
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)
AZ13581837 Related Classifications
HY-115643 Related Classifications
Powered by Bioz