AZD-1656

Names

[ CAS No. ]:
919783-22-5

[ Name ]:
AZD-1656

[Synonym ]:
660M185X4D
3-{[5-(1-Azetidinylcarbonyl)-2-pyrazinyl]oxy}-5-{[(2S)-1-methoxy-2-propanyl]oxy}-N-(5-methyl-2-pyrazinyl)benzamide
AZD1656
Benzamide, 3-[[5-(1-azetidinylcarbonyl)-2-pyrazinyl]oxy]-5-[(1S)-2-methoxy-1-methylethoxy]-N-(5-methyl-2-pyrazinyl)-

Biological Activity

[Description]:

AZD1656 is a potent, selective and orally active glucokinase activator with an EC50 of 60 nM. AZD1656 has the potential for type 2 diabetes research[1][2][3].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Glucokinase

Research Areas >> Metabolic Disease

[Target]

EC50: 60 nM (Glucokinase)[2]

[In Vivo]

AZD1656 (0-9 mg/kg; oral gavage; daily; for 8 weeks; C57BL/6 mice) treatment shows lowered blood glucose and glucose excursion and raised insulin. Liver mRNA levels for various ChREBP target genes including carbohydrate response element binding protein beta isoform (ChREBP-β), G6pc, Pklr, Acly, Acac and Gpd2 are increased by AZD1656[1]. Animal Model: C57BL/6 mice[1] Dosage: 0 mg/kg, 2 mg/kg, 4.5 mg/kg, 9 mg/kg Administration: Oral gavage; daily; for 8 weeks Result: Administered 2 hours before the oral glucose tolerance test, lowered blood glucose and glucose excursion and raised insulin.

[References]

[1]. Brian E Ford, et al. Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge. Diabetes Obes Metab. 2020 Jun 10.

[2]. Medicinal Chemistry, et al. Design and Development of the Glucokinase Activator AZD1656. Complete Accounts of Integrated Drug Discovery and Development: Recent Examples from the Pharmaceutical Industry Volume 1, 185-220.

[3]. Terri Mitchard, et al. The novel use of a heterozygous knockout mouse for embryofetal development assessment of a glucokinase activator. Birth Defects Res B Dev Reprod Toxicol. 2014 Apr;101(2):152-61.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
635.0±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₆N₆O₅

[ Molecular Weight ]:
478.500

[ Flash Point ]:
337.8±31.5 °C

[ Exact Mass ]:
478.196472

[ LogP ]:
-0.21

[ Vapour Pressure ]:
0.0±1.9 mmHg at 25°C

[ Index of Refraction ]:
1.631

[ Storage condition ]:
-20℃

Related Compounds

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