Compounds > azd1656
Page last updated: 2024-11-12

azd1656

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

AZD1656: a glucokinase activator [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID16039797
CHEMBL ID3219124
SCHEMBL ID321593
MeSH IDM0579141

Synonyms (27)

Synonym
azd1656
azd-1656
CHEMBL3219124
azd 1656
3-[5-(azetidine-1-carbonyl)pyrazin-2-yl]oxy-5-[(2s)-1-methoxypropan-2-yl]oxy-n-(5-methylpyrazin-2-yl)benzamide
gtpl7701
SCHEMBL321593
FJEJHJINOKKDCW-INIZCTEOSA-N ,
3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-[(1s)-2-methoxy-1-methylethoxy]-n-(5-methylpyrazin-2-yl)benzamide
660M185X4D ,
azd 1656 [who-dd]
919783-22-5
3-((5-(azetidin-1-ylcarbonyl)pyrazin-2-yl)oxy)-5-((1s)-2-methoxy-1-methylethoxy)-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)-
unii-660m185x4d
E77313
DB14810
Q27074714
HY-15675
(s)-3-(5-(azetidine-1-carbonyl)pyrazin-2-yloxy)-5-(1-methoxypropan-2-yloxy)-n-(5-methylpyrazin-2-yl)benzamide
CS-0008226
MS-28891
cid 16039797
BA171838
AT32772
(s)-3-((5-(azetidine-1-carbonyl)pyrazin-2-yl)oxy)-5-((1-methoxypropan-2-yl)oxy)-n-(5-methylpyrazin-2-yl)benzamide
AKOS040747890

Research Excerpts

Overview

AZD1656 is a novel glucokinase activator with a postulated dual mechanism of action. It has potential to deliver effective glucose-lowering in Type 2 diabetes mellitus.

ExcerptReferenceRelevance
"AZD1656 is a novel glucokinase activator with a postulated dual mechanism of action by activating glucokinase in both the pancreas and the liver, and with the potential to deliver effective glucose-lowering in Type 2 diabetes mellitus. "( Tolerability, pharmacokinetics, and pharmacodynamics of the glucokinase activator AZD1656, after single ascending doses in healthy subjects during euglycemic clamp.
Ericsson, H; Heijer, M; Leonsson-Zachrisson, M; Norjavaara, E; Persson, M; Röshammar, D; Ueda, S; Wollbratt, M, 2012)		2.05

Pharmacokinetics

ExcerptReferenceRelevance
" Safety, pharmacokinetics and pharmacodynamic variables were evaluated."( Safety, pharmacokinetics and pharmacodynamics of multiple-ascending doses of the novel glucokinase activator AZD1656 in patients with type 2 diabetes mellitus.
Ericsson, H; Hompesch, M; Knutsson, M; Leonsson-Zachrisson, M; Morrow, LA; Norjavaara, E; Wollbratt, M, 2012)		0.59
" An active metabolite was formed which had a longer half-life than AZD1656, but showed ∼15% of the area under the plasma concentration versus time curve from 0 to 24 h compared with that of AZD1656."( Safety, pharmacokinetics and pharmacodynamics of multiple-ascending doses of the novel glucokinase activator AZD1656 in patients with type 2 diabetes mellitus.
Ericsson, H; Hompesch, M; Knutsson, M; Leonsson-Zachrisson, M; Morrow, LA; Norjavaara, E; Wollbratt, M, 2012)		0.83
" Taking differences in body weight into account, there were no differences in pharmacokinetic parameters between Western and Japanese subjects."( Tolerability, pharmacokinetics, and pharmacodynamics of the glucokinase activator AZD1656, after single ascending doses in healthy subjects during euglycemic clamp.
Ericsson, H; Heijer, M; Leonsson-Zachrisson, M; Norjavaara, E; Persson, M; Röshammar, D; Ueda, S; Wollbratt, M, 2012)		0.6

Dosage Studied

ExcerptRelevanceReference
" Heterozygous global knockout gkdel/wt females were dosed with 20, 50, or 130 mg/kg/day of AZD1656 or vehicle for a minimum of 14 consecutive days before mating with wild-type males and throughout organogenesis."( The novel use of a heterozygous knockout mouse for embryofetal development assessment of a glucokinase activator.
Mitchard, T; Stewart, J, 2014)		0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (1)

Assay IDTitleYearJournalArticle
AID1226049Antidiabetic activity in C57BL/6J mouse assessed as reduction of blood glucose level at 10 mg/kg, po after 60 mins by fasted glucose tolerance test2015ACS medicinal chemistry letters, Mar-12, Volume: 6, Issue:3
Design and Synthesis of Acetylenyl Benzamide Derivatives as Novel Glucokinase Activators for the Treatment of T2DM.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's9 (90.00)24.3611
2020's1 (10.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 28.43

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index28.43 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index31.18 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (28.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials7 (70.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other3 (30.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
metformin
Metformin: A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289). metformin : A member of the class of guanidines that is biguanide the carrying two methyl substituents at position 1.		4.4422guanidinesenvironmental contaminant;
geroprotector;
hypoglycemic agent;
xenobiotic
pyrazines
Pyrazines: A heterocyclic aromatic organic compound with the chemical formula C4H4N2.. pyrazine : A diazine that is benzene in which the carbon atoms at positions 1 and 4 have been replaced by nitrogen atoms.		8.96108diazine;
pyrazines		Daphnia magna metabolite
sitagliptin
sitagliptin : A triazolopyrazine that exhibits hypoglycemic activity.		2.1110triazolopyrazine;
trifluorobenzene		EC 3.4.14.5 (dipeptidyl-peptidase IV) inhibitor;
environmental contaminant;
hypoglycemic agent;
serine proteinase inhibitor;
xenobiotic
glucagon
Glucagon: A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511). glucagon : A 29-amino acid peptide hormone consisting of His, Ser, Gln, Gly, Thr, Phe, Thr, Ser, Asp, Tyr, Ser, Lys, Tyr, Leu, Asp, Ser, Arg, Arg, Ala, Gln, Asp, Phe, Val, Gln, Trp, Leu, Met, Asn and Thr residues joined in sequence.		9.4322peptide hormone
glucagon-like peptide 1
Glucagon-Like Peptide 1: A peptide of 36 or 37 amino acids that is derived from PROGLUCAGON and mainly produced by the INTESTINAL L CELLS. GLP-1(1-37 or 1-36) is further N-terminally truncated resulting in GLP-1(7-37) or GLP-1-(7-36) which can be amidated. These GLP-1 peptides are known to enhance glucose-dependent INSULIN release, suppress GLUCAGON release and gastric emptying, lower BLOOD GLUCOSE, and reduce food intake.		3.4611
incretins
Incretins: Peptides which stimulate INSULIN release from the PANCREATIC BETA CELLS following oral nutrient ingestion, or postprandially.		3.4611
c-peptide
C-Peptide: The middle segment of proinsulin that is between the N-terminal B-chain and the C-terminal A-chain. It is a pancreatic peptide of about 31 residues, depending on the species. Upon proteolytic cleavage of proinsulin, equimolar INSULIN and C-peptide are released. C-peptide immunoassay has been used to assess pancreatic beta cell function in diabetic patients with circulating insulin antibodies or exogenous insulin. Half-life of C-peptide is 30 min, almost 8 times that of insulin.		3.4611
ConditionIndicatedRelationship StrengthStudiesTrials
2019 Novel Coronavirus Disease
[description not available]		04.6211
Diabetes Mellitus, Adult-Onset
[description not available]		07.5165
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.		19.5165
Hyperglycemia, Postprandial
Abnormally high BLOOD GLUCOSE level after a meal.		04.3911
Hyperglycemia
Abnormally high BLOOD GLUCOSE level.		04.3911
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.110
Fasting Hypoglycemia
HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.		04.4322
Hypoglycemia
A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.		09.4322