AS 1269574
AS 1269574,(2-[2-(4-bromophenyl)-6-methylpyrimidin-4-yl] amino ethanol), was capable of inducing glucose-stimulated insulin secretion (GSIS) and improved glucose tolerance in normal mice. AS 1269574 is an agonist of GPR119 with EC50 value of 2.5 µM [1] [2].
GPR119 is highly expressed in pancreatic β-cells. This receptor enhances the effect of GSIS via the elevation of intracellular cAMP concentrations [2].
Treated with either 1 or 10 µM AS 1269574 for 20 min, the insulin secretion of mouse pancreatic MIN-6 β-cells pre-exposed to 16.8 mM glucose was significantly increased compared with the DMSO vehicle control. In contrast, AS 1269574 did not affect the insulin release of MIN-6 cells previously treated with low-glucose (2.8 mM) [2].
In normal mice, a single treatment with 100 mg/kg of AS 1269574 significantly reduced the area under the curve (AUC) after 2 h (AUC0-2h) of blood glucose. AS 1269574 significantly increase the plasma insulin AUC0-2h in mice compared with the vehicle control. A single oral administration of 100 mg/kg AS 1269574 did not significantly lower the blood glucose AUC in either fasted or fed mice, indicating AS 1269574 did not have a hypoglycemic effect [2].
References:
[1]. Shigeru Yoshida, Hirotsugu Tanaka, Hiroyuki Oshima, et al. AS1907417, a novel GPR119 agonist, as an insulinotropic and β-cell preservative agent for the treatment of type 2 diabetes. Biochemical and Biophysical Research Communications, 2010, 400: 745-751.
[2]. Shigeru Yoshida, Takahide Ohishi, Tetsuo Matsui, et al. Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion. Biochemical and Biophysical Research Communications, 2010, 400: 437-441.
Physical Appearance | A solution in ethanol |
Storage | Store at -20°C |
M.Wt | 308.17 |
Cas No. | 330981-72-1 |
Formula | C13H14BrN3O |
Solubility | Soluble in DMSO |
Chemical Name | 2-((2-(4-bromophenyl)-6-methylpyrimidin-4-yl)amino)ethanol |
SDF | Download SDF |
Canonical SMILES | BrC1=CC=C(C=C1)C2=NC(C)=CC(NCCO)=N2 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
- View current batch:
-
Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
