AS 1269574

Names

[ Name ]:
AS 1269574

[Synonym ]:
hms1581i01
Ethanol, 2-[[2-(4-bromophenyl)-6-methyl-4-pyrimidinyl]amino]-
2-{[2-(4-Bromophenyl)-6-methyl-4-pyrimidinyl]amino}ethanol
AS-1269574

Biological Activity

[Description]:

AS1269574 is a potent, orally available GPR119 agonist, with an EC50 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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel

Signaling Pathways >> GPCR/G Protein >> GPR119

Research Areas >> Metabolic Disease

[Target]

TRPA1

GPR119

[In Vivo]

AS1269574 sgnificantly reduced the blood glucose AUC after 2 h (AUC0-2h) of administration[1]. 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 (AUC0-2h) of administration. Similarly, plasma insulin AUC0-2h was significantly higher in the mice.

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
386.9±42.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₃H₁₄BrN₃O

[ Molecular Weight ]:
308.174

[ Flash Point ]:
187.8±27.9 °C

[ Exact Mass ]:
307.032013

[ PSA ]:
58.04000

[ LogP ]:
2.32

[ Vapour Pressure ]:
0.0±0.9 mmHg at 25°C

[ Index of Refraction ]:
1.648

[ Storage condition ]:
-20℃

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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