| Identification | Back Directory | [Name]
AZD1656 | [CAS]
919783-22-5 | [Synonyms]
AZD1656
AZD-1656
AZD 1656
3-[5-(azetidine-1-carbonyl)pyrazin-2-yl]oxy-5-[(2S)-1-methoxypropan-2-yl]oxy-N-(5-methylpyrazin-2-yl)benzamide
Benzamide, 3-[[5-(1-azetidinylcarbonyl)-2-pyrazinyl]oxy]-5-[(1S)-2-methoxy-1-methylethoxy]-N-(5-methyl-2-pyrazinyl)-
Hexokinase IV,Glucokinase,AZD-1656,AZD1656,G6pc,G6P,ChREBP-β,hypoglycemia,inhibit,Inhibitor,Hexokinase D,epinephrine,glucagon,antihyperglycemic | [Molecular Formula]
C24H26N6O5 | [MDL Number]
MFCD28386282 | [MOL File]
919783-22-5.mol | [Molecular Weight]
478.5 |
| Chemical Properties | Back Directory | [Boiling point ]
635.0±55.0 °C(Predicted) | [density ]
1.336±0.06 g/cm3(Predicted) | [solubility ]
DMSO: Soluble: =10 mg/ml
Ethanol: Slightly soluble: 0.1-1 mg/ml | [form ]
Solid | [pka]
10.84±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [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.
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| [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. DOI:10.1111/dom.14111
[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. DOI:10.1002/bdrb.21102 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
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| Website: |
www.spiropharma.com.cn |
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