330981-72-1 Usage
Uses
Used in Pharmaceutical Industry:
AS 1269574 is used as a therapeutic agent for the treatment of type 2 diabetes and obesity. It works by activating GPR119, which in turn stimulates the secretion of incretin and insulin hormones, helping to regulate blood glucose levels and improve insulin sensitivity.
Used in Research and Development:
AS 1269574 is also used as a research tool for studying the role of GPR119 in glucose homeostasis and its potential as a target for the development of new drugs for the treatment of metabolic disorders.
Biological Activity
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.
Check Digit Verification of cas no
The CAS Registry Mumber 330981-72-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,3,0,9,8 and 1 respectively; the second part has 2 digits, 7 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 330981-72:
(8*3)+(7*3)+(6*0)+(5*9)+(4*8)+(3*1)+(2*7)+(1*2)=141
141 % 10 = 1
So 330981-72-1 is a valid CAS Registry Number.
330981-72-1Relevant academic research and scientific papers
Synthesis and structure-activity relationship of 4-amino-2-phenylpyrimidine derivatives as a series of novel GPR119 agonists
Negoro, Kenji,Yonetoku, Yasuhiro,Maruyama, Tatsuya,Yoshida, Shigeru,Takeuchi, Makoto,Ohta, Mitsuaki
, p. 2369 - 2375 (2012/05/05)
Through preparation and examination of a series of novel 4-amino-2-phenylpyrimidine derivatives as agonists for GPR119, we identified 2-(4-bromophenyl)-6-methyl-N-[2-(1-oxidopyridin-3-yl)ethyl]pyrimidin-4-amine (9t). Compound 9t improved glucose tolerance in mice following oral administration and showed good pharmacokinetic profiles in rats.
