piragliatin profile

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

ID Source	ID
PubMed CID	10432339
CHEMBL ID	1783734
SCHEMBL ID	2642199
MeSH ID	M0552343

Synonym
r04389620
r04389620\\
ro4389620-r1440
ro-4389620
piragliatin
r-1440
D08970
625114-41-2
piragliatin (usan)
tox21_303593
cas-625114-41-2
dtxcid6028494
dtxsid3048520 ,
NCGC00257426-01
(r)-2-(3-chloro-4-(methylsulfonyl)phenyl)-3-((r)-3-oxocyclopentyl)-n-(pyrazin-2-yl)propanamide
chembl1783734 ,
bdbm50346026
(2r)-2-(3-chloro-4-(methylsulfonyl)phenyl)-3-((1r)-3-oxocyclopentyl)-n-pyrazinylpropanamide
bm1hr7ip1l ,
benzeneacetamide, 3-chloro-4-(methylsulfonyl)-alpha-(((1r)-3-oxocyclopentyl)methyl)-n-pyrazinyl-, (alphar)-
piragliatin [usan:inn]
ro4389620
unii-bm1hr7ip1l
ro 4389620
piragliatin [usan]
piragliatin [who-dd]
(2r)-2-[3-chloro-4-(methylsulfonyl)phenyl]-3-[(1r)-3-oxocyclopentyl]-n-pyrazinylpropanamide
ro-4389620-r1440
piragliatin [inn]
2(r)-(3-chloro-4-methanesulfonyl-phenyl)-3-((r)-3-oxo-cyclopentyl)-n-pyrazin-2-yl-propionamide
XEANIURBPHCHMG-SWLSCSKDSA-N
(2r)-2-[3-chloro-4-(methylsulfonyl)phenyl]-3-[(1r)-3-oxocyclopentyl]-n-(pyrazin-2-yl)propanamide
2n8 ,
SCHEMBL2642199
(2r)-2-(3-chloro-4-methylsulfonylphenyl)-3-[(1r)-3-oxocyclopentyl]-n-pyrazin-2-ylpropanamide
Q27274751

Excerpt	Reference	Relevance
"Piragliatin is a CYP3A substrate; its inactive metabolite M4, formed through cytosolic reductase, is reversibly metabolized back to piragliatin through CYP3A. "	( Exploratory effects of a strong CYP3A inhibitor (ketoconazole), a strong CYP3A inducer (rifampicin), and concomitant ethanol on piragliatin pharmacokinetics and pharmacodynamics in type 2 diabetic patients. Boldrin, M; Georgy, A; Liang, Z; Zhai, S; Zhi, J, 2016)	2.08

Excerpt	Reference	Relevance
"Piragliatin was found to lower pre- and postprandial glucose levels, improve the insulin secretory profile, increase β-cell sensitivity to glucose, and decrease hepatic glucose output in patients with T2D."	( Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients. Bizzarro, FT; Corbett, WL; Dvorozniak, MT; Garofalo, L; Geng, W; Grimsby, J; Grippo, JF; Guertin, KR; Haynes, NE; Hilliard, DW; Hutchings, S; Ka, W; Kabat, M; Kester, RF; Liang, Z; Mahaney, PE; Marcus, L; Matschinsky, FM; Moore, D; Pignatello, M; Qi, L; Racha, J; Radinov, R; Ren, Y; Sarabu, R; Spence, CL; Steele, T; Tengi, J, 2012)	1.47

Excerpt	Reference	Relevance
"Piragliatin treatment at steady state yielded dose-dependent reductions up to 32.5% and 35.5% for the highest dose in fasting and postprandial plasma glucose."	( Effects of piragliatin, a glucokinase activator, on fasting and postprandial plasma glucose in patients with type 2 diabetes mellitus. Zhai, S; Zhi, J, 2016)	1.55

Excerpt	Reference	Relevance
" Administration of piragliatin (100-mg single dose) resulted in a 32% Cmax and 44% area under the curve (AUC∞ ) increase in piragliatin exposure without affecting glucose AUC0-6h following ketoconazole (400 mg QD × 5 days); 30% Cmax and 72% AUC∞ decrease in piragliatin exposure with a 13% increase in glucose AUC0-6h following rifampicin (600 mg QD × 5 days); and, unexpectedly, a 32% Cmax and 23% AUC0-6h decrease (no change in AUC∞ ) in piragliatin exposure with a 13% increase in glucose AUC0-6h following alcohol (40-g single dose)."	( Exploratory effects of a strong CYP3A inhibitor (ketoconazole), a strong CYP3A inducer (rifampicin), and concomitant ethanol on piragliatin pharmacokinetics and pharmacodynamics in type 2 diabetic patients. Boldrin, M; Georgy, A; Liang, Z; Zhai, S; Zhi, J, 2016)	0.97
"To evaluate the potential pharmacokinetic (PK) and pharmacodynamic (PD, glucose-lowering effect) interaction between simvastatin and piragliatin, both CYP3A substrates, 30 patients with type 2 diabetes mellitus participated in this open-label, randomized, 6-sequence, 3-way crossover (William's design) study."	( Lack of Potential Pharmacokinetic and Pharmacodynamic Interactions Between Piragliatin, a Glucokinase Activator, and Simvastatin in Patients With Type 2 Diabetes Mellitus. Boldrin, M; Georgy, A; Liang, Z; Zhai, S; Zhi, J, 2016)	0.87
" This clinical pharmacology study was designed to investigate the potential glucose-lowering effect or pharmacodynamic (PD), pharmacokinetic (PK), and safety/tolerability interactions between piragliatin and glyburide in T2D patients already taking glyburide but not adequately controlled."	( Pharmacokinetic and Pharmacodynamic Drug Interaction Study of Piragliatin, a Glucokinase Activator, and Glyburide, a Sulfonylurea, in Type 2 Diabetic Patients. Georgy, A; Liang, Z; Zhai, S; Zhi, J, 2016)	0.86

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Excerpt	Relevance	Reference
" Primary PK and PD parameters were AUCs on dosing days."	( Lack of Potential Pharmacokinetic and Pharmacodynamic Interactions Between Piragliatin, a Glucokinase Activator, and Simvastatin in Patients With Type 2 Diabetes Mellitus. Boldrin, M; Georgy, A; Liang, Z; Zhai, S; Zhi, J, 2016)	0.66

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
acetylcholinesterase	Homo sapiens (human)	Potency	79.6407	0.0025	41.7960	15,848.9004	AID1347395
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	38.8952	0.0002	29.3054	16,493.5996	AID743069
peroxisome proliferator-activated receptor delta	Homo sapiens (human)	Potency	8.7076	0.0010	24.5048	61.6448	AID743215
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	24.3365	0.0006	27.2152	1,122.0200	AID743202
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Hexokinase-4	Homo sapiens (human)	EC50 (µMol)	3.8700	0.0900	1.2687	6.3200	AID1276628; AID600093
Hexokinase-4	Homo sapiens (human)	Kd	0.8300	0.5000	0.6650	0.8300	AID1628602
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Hexokinase-4	Homo sapiens (human)	Activity	0.1800	0.1270	0.1823	0.2400	AID698011
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
glucose catabolic process	Hexokinase-4	Homo sapiens (human)
regulation of glycolytic process	Hexokinase-4	Homo sapiens (human)
NADP metabolic process	Hexokinase-4	Homo sapiens (human)
response to glucose	Hexokinase-4	Homo sapiens (human)
positive regulation of insulin secretion	Hexokinase-4	Homo sapiens (human)
cellular response to insulin stimulus	Hexokinase-4	Homo sapiens (human)
glucose homeostasis	Hexokinase-4	Homo sapiens (human)
regulation of potassium ion transport	Hexokinase-4	Homo sapiens (human)
cellular response to leptin stimulus	Hexokinase-4	Homo sapiens (human)
negative regulation of gluconeogenesis	Hexokinase-4	Homo sapiens (human)
positive regulation of glycogen biosynthetic process	Hexokinase-4	Homo sapiens (human)
regulation of insulin secretion	Hexokinase-4	Homo sapiens (human)
glucose 6-phosphate metabolic process	Hexokinase-4	Homo sapiens (human)
canonical glycolysis	Hexokinase-4	Homo sapiens (human)
calcium ion import	Hexokinase-4	Homo sapiens (human)
glucose metabolic process	Hexokinase-4	Homo sapiens (human)
intracellular glucose homeostasis	Hexokinase-4	Homo sapiens (human)
glycolytic process	Hexokinase-4	Homo sapiens (human)
carbohydrate phosphorylation	Hexokinase-4	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
glucokinase activity	Hexokinase-4	Homo sapiens (human)
protein binding	Hexokinase-4	Homo sapiens (human)
ATP binding	Hexokinase-4	Homo sapiens (human)
glucose binding	Hexokinase-4	Homo sapiens (human)
glucose sensor activity	Hexokinase-4	Homo sapiens (human)
fructokinase activity	Hexokinase-4	Homo sapiens (human)
mannokinase activity	Hexokinase-4	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
nucleoplasm	Hexokinase-4	Homo sapiens (human)
cytosol	Hexokinase-4	Homo sapiens (human)
mitochondrion	Hexokinase-4	Homo sapiens (human)
cytosol	Hexokinase-4	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (127)

Assay ID	Title	Year	Journal	Article
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID698012	Drug degradation in Sprague-Dawley rat liver microsomes assessed as formation of metabolite 1 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698361	AUC (0 to infinity) in monkey at 5 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405568	Antidiabetic activity in C57BL/6J mouse assessed as increase in insulin secretion at 30 mg/kg, po measured up to 60 mins by ELISA	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698213	Drug metabolism in beagle dog liver microsomes at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1628607	Displacement of TAFMT from human pancreatic N-terminal His6-tagged glucokinase isoform 1 expressed in Escherichia coli BL21(DE3) assessed as compound association rate constant by stopped-flow fluorometric method	2016	Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15	Molecular Dynamics Simulations and Kinetic Measurements to Estimate and Predict Protein-Ligand Residence Times.
AID1405578	AUC (0 to 1.5 hrs) in C57BL/6J mouse plasma at 30 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698351	Plasma clearance in monkey at 5 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698362	AUC (0 to infinity) in dog at 30 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698206	Cardiotoxicity in dog assessed as prolongation of QT interval	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID697996	Drug degradation in human liver microsomes assessed as formation of metabolite 2 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID697998	Metabolic stability in CD1 mouse liver microsomes assessed as concentration of parent compound at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698205	Activity at human recombinant glucokinase assessed as increase in Vmax at 1 uM	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698349	Volume of distribution at steady state in mouse at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698366	AUC (0 to infinity) in mouse at 30 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1276633	Antihyperglycemic effect in fasted C57BL/6J mouse assessed as blood glucose level at 45 mg/kg, po measured at 2 hrs by glucometry analysis (Rvb = 9.1 to 9.5 mM)	2016	Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2	Structure-Activity Relationship of Azaindole-Based Glucokinase Activators.
AID1405592	Ratio of AUC (0 to 1.5 hrs) in C57BL/6J mouse pancreas to plasma at 10 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698350	Volume of distribution at steady state in rat at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698002	Activation of human recombinant glucokinase	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698027	Drug degradation in cynomolgus monkey liver microsomes assessed as formation of metabolite 2 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405581	AUC (0 to 1.5 hrs) in C57BL/6J mouse liver at 30 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698172	Tmax in mouse at 60 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID697994	Drug degradation in Beagle dog liver microsomes assessed as formation of metabolite 2 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698022	Drug degradation in human liver microsomes assessed as formation of metabolite 1 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698157	Drug degradation in human liver microsomes assessed as formation of metabolite 5 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698212	Drug metabolism in cynomolgus monkey liver microsomes at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405597	Ratio of AUC (0 to 1.5 hrs) in C57BL/6J mouse liver to pancreas at 30 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698186	Antidiabetic activity in po dosed DIO C57Bl/6J mouse assessed as reduction of glucose excursion administered 1 hr before glucose challenge measured after 2 hrs by OGTT	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698016	Drug degradation in cynomolgus monkey liver microsomes assessed as formation of metabolite 1 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698026	Drug degradation in cynomolgus monkey liver microsomes assessed as formation of metabolite 3 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698173	Tmax in rat at 30 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405588	Ratio of AUC (0 to 1.5 hrs) in C57BL/6J mouse liver to plasma at 10 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698170	Cmax in monkey at 5 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698164	Cmax in rat at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698000	Metabolic stability in human liver microsomes assessed as concentration of parent compound at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405584	AUC (0 to 1.5 hrs) in C57BL/6J mouse pancreas at 10 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698176	Tmax in monkey at 5 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698352	Plasma clearance in dog at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698200	Plasma protein binding in dog	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID734300	Metabolic stability in human hepatocytes after 3 hrs by LC-MS/MS analysis	2013	ACS medicinal chemistry letters, Apr-11, Volume: 4, Issue:4	Identification of RO4597014, a Glucokinase Activator Studied in the Clinic for the Treatment of Type 2 Diabetes.
AID698009	Drug degradation in Sprague-Dawley rat liver microsomes assessed as formation of metabolite 3 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698217	Drug degradation in CD1 mouse liver microsomes assessed as formation of metabolite 5 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1628609	Displacement of TAFMT from human pancreatic N-terminal His6-tagged glucokinase isoform 1 expressed in Escherichia coli BL21(DE3) assessed as compound dissociation rate constant by stopped-flow fluorometric method	2016	Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15	Molecular Dynamics Simulations and Kinetic Measurements to Estimate and Predict Protein-Ligand Residence Times.
AID1405575	AUC (0 to 1.5 hrs) in C57BL/6J mouse liver at 10 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698364	AUC (0 to infinity) in rat at 60 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698202	Hepatic toxicity in Wistar rat assessed as lipidosis at 120 mg/kg, po qd for 4 weeks by Oil Red O staining	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698003	Distribution coefficient, log D of the compound at pH 7.4	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698167	Cmax in dog at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405599	Ratio of AUC (0 to 1.5 hrs) in C57BL/6J mouse liver to pancreas at 5 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698162	Cmax in mouse at 30 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698214	Drug metabolism in human liver microsomes at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1276632	Antihyperglycemic effect in fasted C57BL/6J mouse assessed as reduction in blood glucose level at 45 mg/kg, po measured after 4 hrs by glucometry analysis	2016	Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2	Structure-Activity Relationship of Azaindole-Based Glucokinase Activators.
AID698166	Cmax in rat at 60 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405585	AUC (0 to 1.5 hrs) in C57BL/6J mouse pancreas at 30 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID697997	Drug degradation in human liver microsomes assessed as formation of metabolite 3 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405593	Ratio of AUC (0 to 1.5 hrs) in C57BL/6J mouse pancreas to plasma at 30 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698175	Tmax in dog at 30 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1628608	Activation of human pancreatic N-terminal His6-tagged glucokinase isoform 1 expressed in Escherichia coli BL21(DE3) assessed as conversion of glucose to glucose-6-phosphate by G6PDH/NADP-coupled enzyme assay	2016	Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15	Molecular Dynamics Simulations and Kinetic Measurements to Estimate and Predict Protein-Ligand Residence Times.
AID698181	Oral bioavailability in dog at 30 mg/kg	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698019	Drug degradation in cynomolgus monkey liver microsomes assessed as formation of metabolite 5 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698179	Oral bioavailability in rat at 30 mg/kg	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698355	Drug degradation in CD1 mouse liver microsomes assessed as formation of metabolite 2 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698353	Volume of distribution at steady state in monkey at 5 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698174	Tmax in rat at 60 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698354	Plasma clearance in rat at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698363	AUC (0 to infinity) in dog at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698169	Cmax in monkey at 5 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID600093	Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophotometry	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle.
AID697995	Drug degradation in Beagle dog liver microsomes assessed as formation of metabolite 3 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405583	AUC (0 to 1.5 hrs) in C57BL/6J mouse liver at 5 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID697993	Metabolic stability in cynomolgus monkey liver microsomes assessed as concentration of parent compound at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698365	AUC (0 to infinity) in rat at 30 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698207	Activity at human recombinant glucokinase assessed as decrease in Km at 1 uM	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698168	Cmax in dog at 30 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405596	Ratio of AUC (0 to 1.5 hrs) in C57BL/6J mouse liver to pancreas at 10 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698004	Plasma protein binding in human	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698171	Tmax in mouse at 30 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698187	Antidiabetic activity in po dosed DIO C57Bl/6J mouse assessed as reduction of glucose excursion administered 1 hr before glucose challenge measured after 4 hrs by OGTT	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698356	Metabolic stability in Sprague-Dawley rat liver microsomes assessed as concentration of parent compound at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405587	AUC (0 to 1.5 hrs) in C57BL/6J mouse pancreas at 5 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698360	AUC (0 to infinity) in monkey at 5 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698153	Drug degradation in Beagle dog liver microsomes assessed as formation of metabolite 5 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698178	Oral bioavailability in mouse at 60 mg/kg	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698198	Plasma protein binding in mouse	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698177	Oral bioavailability in mouse at 30 mg/kg	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698188	Volume of distribution at steady state in dog at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698184	Drug excretion iv dosed rat urine after 72 hrs	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698201	Plasma protein binding in monkey	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698183	Drug excretion iv dosed rat feces after 72 hrs	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698163	Cmax in mouse at 60 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698180	Oral bioavailability in rat at 60 mg/kg	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698348	AUC (0 to infinity) in rat at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698161	Cmax in mouse at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405573	Toxicity in C57BL/6J mouse assessed as hypoglycemia at 30 mg/kg, po measured up to 300 mins by glucometric method	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID1628610	Displacement of TAFMT from human pancreatic N-terminal His6-tagged glucokinase isoform 1 expressed in Escherichia coli BL21(DE3) assessed as compound residence time by stopped-flow fluorometric method	2016	Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15	Molecular Dynamics Simulations and Kinetic Measurements to Estimate and Predict Protein-Ligand Residence Times.
AID1405567	Antidiabetic activity in po dosed C57BL/6J mouse assessed as reduction in blood glucose level administered for 15 to 30 mins prior to glucose challenge measured up to 120 mins post dose by OGTT	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698028	Drug degradation in CD1 mouse liver microsomes assessed as formation of metabolite 3 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698025	Drug degradation in CD1 mouse liver microsomes assessed as formation of metabolite 1 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405595	Ratio of AUC (0 to 1.5 hrs) in C57BL/6J mouse pancreas to plasma at 5 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698007	Drug degradation in Sprague-Dawley rat liver microsomes assessed as formation of metabolite 5 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1628602	Displacement of TAFMT from human pancreatic N-terminal His6-tagged glucokinase isoform 1 expressed in Escherichia coli BL21(DE3) by stopped-flow fluorometric method	2016	Journal of medicinal chemistry, 08-11, Volume: 59, Issue:15	Molecular Dynamics Simulations and Kinetic Measurements to Estimate and Predict Protein-Ligand Residence Times.
AID1405591	Ratio of AUC (0 to 1.5 hrs) in C57BL/6J mouse liver to plasma in C57BL/6J mouse at 5 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID1276635	Stability in C57BL/6J mouse microsomes	2016	Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2	Structure-Activity Relationship of Azaindole-Based Glucokinase Activators.
AID698358	Apparent permeability across human Caco2 cells	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405589	Ratio of AUC (0 to 1.5 hrs) in C57BL/6J mouse liver to plasma at 30 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698359	Solubility of the compound	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698357	Intrinsic clearance in human hepatocytes	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698185	Antidiabetic activity in DIO C57Bl/6J mouse assessed as reduction of glucose excursion at 5 to 15 mg/kg, po administered 1 hr before glucose challenge measured up to 120 mins by OGTT	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1276629	Activation of recombinant human glucokinase assessed as NADPH formation using glucose as substrate incubated for 30 mins in presence of NADP+ and glucose 6-phosphate dehydrogenase relative to control	2016	Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2	Structure-Activity Relationship of Azaindole-Based Glucokinase Activators.
AID698032	Drug degradation in Beagle dog liver microsomes assessed as formation of metabolite 1 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698208	Inhibition of CYP P450	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID600094	Activation of human recombinant glucokinase using 6.5 mM glucose by spectrophotometry relative to control	2009	Bioorganic & medicinal chemistry letters, Jun-15, Volume: 19, Issue:12	Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle.
AID698010	Drug degradation in Sprague-Dawley rat liver microsomes assessed as formation of metabolite 2 at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698347	Plasma clearance in mouse at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698182	Oral bioavailability in monkey at 5 mg/kg	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID697999	Metabolic stability in Beagle dog liver microsomes assessed as concentration of parent compound at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698367	AUC (0 to infinity) in mouse at 10 mg/kg, iv	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405577	AUC (0 to 1.5 hrs) in C57BL/6J mouse plasma at 10 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698165	Cmax in rat at 30 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1405580	AUC (0 to 1.5 hrs) in C57BL/6J mouse plasma at 5 mg/kg, po administered as single dose by LC/MS/MS analysis	2018	European journal of medicinal chemistry, Aug-05, Volume: 156	Discovery of a potent glucokinase activator with a favorable liver and pancreas distribution pattern for the treatment of type 2 diabetes mellitus.
AID698199	Plasma protein binding in rat	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698210	Drug metabolism in CD1 mouse liver microsomes at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698011	Activation of human recombinant glucokinase assessed as concentration required for 1.5 fold increase in enzymatic activity	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID698211	Drug metabolism in Sprague-Dawley rat liver microsomes at 20 uM after 30 mins by LCMS/MS analysis	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
AID1276628	Activation of recombinant human glucokinase assessed as NADPH formation using glucose as substrate incubated for 30 mins in presence of NADP+ and glucose 6-phosphate dehydrogenase	2016	Journal of medicinal chemistry, Jan-28, Volume: 59, Issue:2	Structure-Activity Relationship of Azaindole-Based Glucokinase Activators.
AID698346	AUC (0 to infinity) in mouse at 60 mg/kg, po	2012	Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16	Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	1 (5.26)	29.6817
2010's	18 (94.74)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	6 (31.58%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	13 (68.42%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
glyburide Glyburide: An antidiabetic sulfonylurea derivative with actions like those of chlorpropamide. glyburide : An N-sulfonylurea that is acetohexamide in which the acetyl group is replaced by a 2-(5-chloro-2-methoxybenzamido)ethyl group.	8.51	1	1	monochlorobenzenes; N-sulfonylurea	anti-arrhythmia drug; EC 2.7.1.33 (pantothenate kinase) inhibitor; EC 3.6.3.49 (channel-conductance-controlling ATPase) inhibitor; hypoglycemic agent
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	8.51	1	1	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
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.	3.51	1	1	guanidines	environmental contaminant; geroprotector; hypoglycemic agent; xenobiotic
simvastatin Simvastatin: A derivative of LOVASTATIN and potent competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES), which is the rate-limiting enzyme in cholesterol biosynthesis. It may also interfere with steroid hormone production. Due to the induction of hepatic LDL RECEPTORS, it increases breakdown of LDL CHOLESTEROL.. simvastatin : A member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.	8.51	1	1	delta-lactone; fatty acid ester; hexahydronaphthalenes; statin (semi-synthetic)	EC 1.1.1.34/EC 1.1.1.88 (hydroxymethylglutaryl-CoA reductase) inhibitor; EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor; ferroptosis inducer; geroprotector; prodrug
moxifloxacin Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent.. moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents.	3.53	1	1	aromatic ether; cyclopropanes; fluoroquinolone antibiotic; pyrrolidinopiperidine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone	antibacterial drug
benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.	2.1	1	0
glycogen glycogen : A polydisperse, highly branched glucan composed of chains of D-glucopyranose residues in alpha(1->4) glycosidic linkage, joined together by alpha(1->6) glycosidic linkages. A small number of alpha(1->3) glycosidic linkages and some cumulative alpha(1->6) links also may occur. The branches in glycogen typically contain 8 to 12 glucose residues.	2.08	1	0
ro-28-1675 [no description available]	2.46	2	0	acetamides
sitagliptin phosphate Sitagliptin Phosphate: A pyrazine-derived DIPEPTIDYL-PEPTIDASE IV INHIBITOR and HYPOGLYCEMIC AGENT that increases the levels of the INCRETIN hormones GLUCAGON-LIKE PEPTIDE-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). It is used in the treatment of TYPE 2 DIABETES.	3.51	1	1
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.	2.07	1	0
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.	5.79	2	2
pf-04279405 PF-04279405: a glucokinase activator	2.1	1	0
exenatide Exenatide: A synthetic form of exendin-4, a 39-amino acid peptide isolated from the venom of the Gila monster lizard (Heloderma suspectum). Exenatide increases CYCLIC AMP levels in pancreatic acinar cells and acts as a GLUCAGON-LIKE PEPTIDE-1 RECEPTOR (GLP-1) agonist and incretin mimetic, enhancing insulin secretion in response to increased glucose levels; it also suppresses inappropriate glucagon secretion and slows gastric emptying. It is used an anti-diabetic and anti-obesity agent.	7.77	3	0
pf-04937319 N,N-dimethyl-5-((2-methyl-6-((5-methylpyrazin-2-yl)carbamoyl)benzofuran-4-yl)oxy)pyrimidine-2-carboxamide: a glucokinase activator; structure in first source	2.1	1	0
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	3.51	1	1	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor

Condition	Relationship Strength	Studies	Trials
Diabetes Mellitus, Adult-Onset [description not available]	9.32	13	9
Lipidoses Conditions characterized by abnormal lipid deposition due to disturbance in lipid metabolism, such as hereditary diseases involving lysosomal enzymes required for lipid breakdown. They are classified either by the enzyme defect or by the type of lipid involved.	2.07	1	0
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.	9.32	13	9
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	2.08	1	0
Liver Steatosis [description not available]	2.08	1	0
Hyperglycemia, Postprandial Abnormally high BLOOD GLUCOSE level after a meal.	2.08	1	0
Insulin Sensitivity [description not available]	2.08	1	0
Fatty Liver Lipid infiltration of the hepatic parenchymal cells resulting in a yellow-colored liver. The abnormal lipid accumulation is usually in the form of TRIGLYCERIDES, either as a single large droplet or multiple small droplets. Fatty liver is caused by an imbalance in the metabolism of FATTY ACIDS.	2.08	1	0
Hyperglycemia Abnormally high BLOOD GLUCOSE level.	2.08	1	0
Insulin Resistance Diminished effectiveness of INSULIN in lowering blood sugar levels: requiring the use of 200 units or more of insulin per day to prevent HYPERGLYCEMIA or KETOSIS.	2.08	1	0
Fasting Hypoglycemia HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.	2.1	1	0
Peripheral Nerve Diseases [description not available]	2.1	1	0
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.	2.1	1	0
Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.	2.1	1	0
Peripheral Nervous System Diseases Diseases of the peripheral nerves external to the brain and spinal cord, which includes diseases of the nerve roots, ganglia, plexi, autonomic nerves, sensory nerves, and motor nerves.	2.1	1	0

piragliatin

Description

Cross-References

Synonyms (36)

Research Excerpts

Overview

Actions

Treatment

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (5)

Potency Measurements

Activation Measurements

Other Measurements

Biological Processes (19)

Molecular Functions (7)

Ceullar Components (3)

Bioassays (127)

Research

Studies (19)

Market Indicators

Research Demand Index: 23.96

Study Types

piragliatin

Description

Cross-References

Synonyms (36)

Research Excerpts

Overview

Actions

Treatment

Pharmacokinetics

Bioavailability

Dosage Studied

Protein Targets (5)

Potency Measurements

Activation Measurements

Other Measurements

Biological Processes (19)

Molecular Functions (7)

Ceullar Components (3)

Bioassays (127)

Research

Studies (19)

Market Indicators

Research Demand Index: 23.96

Study Types

Related Drugs (15)

Related Conditions (15)