[CAS NO. 330981-72-1] AS1269574
PRODUCTS SPECIFICATIONS [330981-72-1]
DESCRIPTION [330981-72-1]
Overview
| MDL | MFCD00298280 |
|---|---|
| Molecular Weight | 308.17 |
| Molecular Formula | C13H14BrN3O |
| SMILES | OCCNC1=NC(C2=CC=C(Br)C=C2)=NC(C)=C1 |
Summary
AS1269574 is a potent, orally available GPR119 agonist, with an EC 50 of 2.5 μM in HEK293 cells expressing human GPR119 . AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes [1] [2] .
IC50 & Target
|
GPR119 |
TRPA1 |
In Vivo
AS1269574 sgnificantly reduced the blood glucose AUC after 2 h (AUC 0-2h ) of administration [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Eight-week-old ICR mice [1] |
| Dosage: | 100 mg/kg |
| Administration: | P.o. |
| Result: | Sgnificantly reduced the blood glucose AUC after 2 h (AUC 0-2h ) of administration. Similarly, plasma insulin AUC 0-2h was significantly higher in the mice. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 250 mg/mL ( 811.24 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2450 mL | 16.2248 mL | 32.4496 mL |
| 5 mM | 0.6490 mL | 3.2450 mL | 6.4899 mL |
| 10 mM | 0.3245 mL | 1.6225 mL | 3.2450 mL |
References
- [1] Yoshida S, et al. Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochem Biophys Res Commun. 2010;400(3):437-441.
- [2] Chepurny OG, et al. GPR119 Agonist AS1269574 Activates TRPA1 Cation Channels to Stimulate GLP-1 Secretion. Mol Endocrinol. 2016;30(6):614-629.