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AZD-1656

Catalog No. T26712 CAS 919783-22-5

Synonyms: AZD 1656

AZD-1656 is a glucokinase activator (GKA) that can cause dose-limiting hypoglycemia in normal animals used in embryofetal development studies and type 2 diabetes.

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AZD-1656, CAS 919783-22-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 116.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 462.00
25 mg	In stock	$ 793.00
50 mg	In stock	$ 1,080.00
1 mL * 10 mM (in DMSO)	In stock	$ 329.00

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Purity: 99.37%

Biological Description

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Description	AZD-1656 is a glucokinase activator (GKA) that can cause dose-limiting hypoglycemia in normal animals used in embryofetal development studies and type 2 diabetes.
Targets&IC50	GK:60 nM (EC50)
In vivo	The gkdel/wt mouse was used as an alternative rodent strain for embryofetal development studies with AZD-1656. Heterozygous global knockout gkdel/wt females were dosed with 20, 50, or 130 mg/kg/day of AZD-1656 or vehicle for a minimum of 14 consecutive days before mating with wild-type males and throughout organogenesis. Maternal effects were confined to slightly reduced food consumption, reduced body weight gain, and the pharmacologic effect of decreased plasma glucose. Fetuses were genotyped. Fetal weights at the high dose were slightly reduced but there was no effect on fetal survival. There were two specificmajormalformations, omphalocele and right-sided aortic arch, with increased fetal incidence in mid- and high-dose fetuses (e.g., omphalocele fetal incidence of 0.6, 0.7, 4.6, and 2% across the dose groups) plus increased incidences of minor abnormalities and variants indicative of either delayed or disturbed development. Fetal weight and abnormalities were unaffected by fetal genotype. The fetal effects are considered hypoglycemia related. There was no effect on embryofetal survival in the gkdel/wt mouse at AZD-1656 exposures[1].

Synonyms	AZD 1656
Molecular Weight	478.5
Formula	C24H26N6O5
CAS No.	919783-22-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (522.47 mM)

References and Literature

1. Krentz AJ, et al. Effect of exogenously administered glucagon versus spontaneous endogenous counter-regulation on glycaemic recovery from insulin-induced hypoglycaemia in patients with type 2 diabetes treated with a novel glucokinase activator, AZD1656, and metformin. Diabetes Obes Metab. 2014 Nov;16(11):1096-101. 2. 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. 3. 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. 4. 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.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Drug Repurposing Compound Library Bioactive Compound Library Clinical Compound Library Orally Active Compound Library Anti-Cancer Metabolism Compound Library Glycolysis Compound Library Anti-Viral Compound Library Metabolism Compound Library Bioactive Compounds Library Max

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Keywords

AZD-1656 919783-22-5 Metabolism Glucokinase Hexokinase IV AZD1656 G6pc G6P ChREBP-β hypoglycemia AZD 1656 inhibit Inhibitor Hexokinase D epinephrine glucagon antihyperglycemic inhibitor

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