AS1535907
AS1535907 is an orally active GPR119 agonist with an EC50 of 1.5 μM in HEK293 cells. AS1535907 activates GPR119, driving dose-dependent intracellular cAMP accumulation and Glucose (D-Glucose) (HY-B0389)-stimulated insulin secretion. AS1535907 lowers blood glucose and increases early plasma insulin levels in diabetic mice. AS1535907 protects pancreatic β-cell function and islet structure. AS1535907 can be used for research on type 2 diabetes.
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- CAS. Nr.: 504402-21-5
- Formel: C18H17BrN4O
- Molecular Weight:385.26
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
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GPR119 1.5 μM (EC50) |
In Vitro
AS1535907 (10 μM) enhances first-phase insulin secretion in isolated perfused rat pancreas under 16.8 mM Glucose conditions and does not affect secretion under 2.8 mM Glucose conditions[1].
AS1535907 (10 μM; 30 min) enhances glucose-stimulated insulin secretion in NIT-1 cells exposed to 16.8 mM Glucose[2].
AS1535907 (0.01-30 μM; 24 h) increases human insulin promoter-driven luciferase activity in NIT-1 cells within the 0.01-30 μM range[2].
AS1535907 (10 μM; 30-40 min) enhances first-phase glucose-stimulated insulin secretion in isolated perfused pancreas of GK rats[2].
AS1535907 (0.01-100 μM; 15 min) acts as a human GPR119 agonist in HEK293 cells with an EC50 of 1.5 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AS1535907 (10 mg/kg; p.o.; single administration; administered 30 min before oral Glucose) improves oral Glucose tolerance and the early plasma insulin response in normal ICR mice[2].
AS1535907 (10 mg/kg; p.o.; twice daily; 2 weeks) improves oral Glucose tolerance and the early plasma insulin response in db/db mice[2].
AS1535907 (10-30 mg/kg; p.o.; twice daily; 2 weeks) reduces blood glucose and increases plasma and pancreatic insulin and insulin mRNA levels in db/db mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:db/db (male, 6 weeks old)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single administration; 30 min before oral Glucose challenge
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Result:Produced a clear decrease in blood Glucose during the OGTT compared with vehicle, with reduced blood Glucose AUC0-0.5 h and AUC0-3 h.
Also increased early-phase plasma insulin; plasma insulin at 5 min and plasma insulin AUC0-10 min were higher than with vehicle.
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Animal Model:ICR (male, 6 weeks old)[2]
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Dosage:10 mg/kg
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Administration:p.o.; single dose; 30 min before oral Glucose
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Result:At 10 mg/kg, blood Glucose AUC0-60 min was lower than vehicle.
At 10 mg/kg, plasma insulin AUC0-15 min was higher than vehicle.
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Animal Model:db/db (male, 6 weeks old)[2]
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Dosage:10 mg/kg
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Administration:p.o.; twice daily; 2 weeks
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Result:At 10 mg/kg twice daily for 2 weeks, blood Glucose AUC0-180 min was lower than vehicle.
At 10 mg/kg twice daily for 2 weeks, plasma insulin AUC0-30 min was higher than vehicle.
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Animal Model:db/db (male, 6 weeks old)[2]
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Dosage:10 mg/kg and 30 mg/kg
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Administration:p.o.; twice daily; 2 weeks
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Result:At 10 mg/kg twice daily for 2 weeks, blood Glucose and plasma insulin levels improved versus vehicle.
At 30 mg/kg twice daily for 2 weeks, blood Glucose was lower than nateglinide and glibenclamide.
At 30 mg/kg twice daily for 2 weeks, plasma insulin and pancreatic insulin were higher than nateglinide and glibenclamide.
At 30 mg/kg twice daily for 2 weeks, pancreatic insulin mRNA was higher than vehicle.
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Animal Model:db/db (male, 6 weeks old)[2]
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Dosage:30 mg/kg
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Administration:p.o.; 3 weeks
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Result:At 30 mg/kg, insulin-positive and PCNA-positive cell numbers and islet area were higher than vehicle.
At 30 mg/kg, insulin, Nkx2.2, Nkx6.1, NeuroD, and PC1 expression were higher than vehicle.
At 30 mg/kg, increases in PDX-1, HNF1α, and activin expression were not significant.
Chemical Information
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CAS. Nr. 504402-21-5
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Molecular Weight 385.26
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Formel C18H17BrN4O
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SMILES
[O-][N+]1=CC(CCNC2=NC(C3=CC=C(Br)C=C3)=NC(C)=C2)=CC=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Yoshida S, et al. Novel GPR119 agonist AS1535907 contributes to first-phase insulin secretion in rat perfused pancreas and diabetic db/db mice. Biochemical and biophysical research communications. 2010 Nov 12;402(2):280-5. [Content Brief]
[2]. Yoshida S, et al. The role of small molecule GPR119 agonist, AS1535907, in glucose-stimulated insulin secretion and pancreatic β-cell function. Diabetes, obesity & metabolism. 2011 Jan;13(1):34-41. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AS1535907 Related Classifications
HY-189086 Related Classifications
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Keywords
- AS1535907
- 504402-21-5
- AS 1535907
- AS-1535907
- GPR119
- G Protein-Coupled Receptor 119
- GPR119 agonist
- first-phase insulin secretion
- glucose-stimulated insulin secretion
- incretin release
- insulin mRNA
- intracellular cAMP accumulation
- islet structure
- oral glucose tolerance
- pancreatic β-cell
- type 2 diabetes mellitus
- Inhibitor
- inhibitor
- inhibit