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Glucokinase activators act on hexokinase IV, the glucose sensor of pancreatic beta cells and the liver. Glucokinase (GK) phosphorylates glucose to glucose-6-phosphate with low affinity and without inhibition by its product. Its activity therefore rises and falls with blood glucose over the physiological range. A 1995 study of knockout mice showed that beta-cell glucokinase is required to maintain glucose homeostasis. In 2003 Ro 28-1675 was described as an allosteric activator that binds outside the active site and increases glucose affinity. Later activators in the catalogue include piragliatin, MK-0941 and globalagliatin. PF-04991532 is a hepatoselective activator used to separate liver effects from those in islets.
Synonyms: LY-2608204
LY2608204 is a potent used to treat type 2 diabetes. In a clinical trial, a study was performed to evaluate the safety and tolerability of LY2608204 in patients with type 2 diabetes.
PF-04991532 is a potent, hepatoselective glucokinase activator with EC50s of 80 and 100 nM in human and rat, respectively.
Synonyms: PF04937319
PF-04937319 is a glucokinase activator (GKA) with EC50 value of 154.4 μM, one of the most promising strategies for the treatment of type 2 diabetes mellitus.
Synonyms: RO4389620; R 1440
Piragliatin is a novel glucokinase activator, lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus
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Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.
AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.
MK-0941 is a potent, orally active and allosteric glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 has potential in the treatment of type 2 diabetes.
Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM.
ML266 (CID-46943215) is a activator of glucocerebrosidase (GCase) that does not inhibit the enzyme’s action but can still facilitates its translocation to the lysosome.
Synonyms: HMS5552
Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes.
NVP-LBX192 is a potent glucokinase activator with a K(a) of 39 nM. This compound effectively lowers glucose levels, making it an important tool for studying metabolic diseases, particularly type 2 diabetes. Researchers can utilize NVP-LBX192 to explore its therapeutic potential and mechanisms of action in glucose homeostasis and insulin sensitivity.
AZD1656 is a potent and selective glucokinase activator that exhibits an EC50 of 60 nM. This compound has significant potential for research involving type 2 diabetes by enhancing glucose metabolism and insulin secretion. It serves as a valuable tool in studies aimed at understanding glucose homeostasis and therapeutic strategies for managing diabetes.
BMS-820132 is a partial glucokinase (GK) activator with an AC50 of 29 nM, demonstrating oral bioactivity. It effectively lowers glucose levels in the oral glucose tolerance test (OGTT) in normal rats, but does not produce the same effect in Zucker diabetic fatty (ZDF) rats. Due to its potent GK activation, BMS-820132 may have associated pharmacological toxicity, highlighting its potential use in research related to metabolic disorders and glucose regulation.
AR453588 is a potent glucokinase activator that demonstrates an EC50 of 42 nM. This compound exhibits significant anti-hyperglycemic activity, making it valuable for research into diabetes and metabolic disorders. Its oral bioavailability further supports its utility in preclinical studies aimed at evaluating glucokinase modulation for therapeutic interventions.
MK-0941 free base is a potent glucokinase activator that enhances the activity of glucokinase, exhibiting EC50 values of 240 nM and 65 nM in the presence of 2.5 mM and 10 mM glucose, respectively. This compound demonstrates significant glucose-lowering effects, highlighting its potential as a therapeutic agent for the treatment of type 2 diabetes. MK-0941 free base is valuable for research into metabolic disorders and the regulation of glucose homeostasis.
AR453588 hydrochloride is a potent glucokinase activator with an EC50 of 42 nM. This compound exhibits significant anti-hyperglycemic activity, making it a valuable tool for research in diabetes and metabolic disorders. Its oral bioavailability enhances its potential for in vivo studies, facilitating exploration of glucokinase modulation in glucose metabolism.
Glucokinase activator 6 is a potent activator of glucokinase, exhibiting an EC50 of 0.09 μM. This compound is primarily utilized in research related to type 2 diabetes (T2D), aiming to enhance glucose metabolism and insulin sensitivity. Its application in metabolic studies makes it an essential tool for investigating therapeutic strategies in T2D management.
Synonyms: NVP-LCZ960
LCZ960 is an orally active glucokinase (GK) activator that enhances GK activity in hepatocytes in vitro and promotes glucose uptake in vivo. This compound effectively lowers blood glucose levels in diet-induced obesity (DIO) models, helping to maintain normoglycemia and improve glucose tolerance in both mice and rats. Additionally, LCZ960 stimulates glycogen synthase activity and enhances hepatic glycogen turnover, making it a valuable tool for researchers studying high-fat diet-induced obesity and type 2 diabetes mechanisms.
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AZD1092 is an orally active glucokinase (GK) activator with an EC50 value of 0.03 μM. It enhances glycolysis and insulin secretion, making it a valuable tool in the study of Type 2 Diabetes (T2D) and related metabolic disorders. Its role in modulating blood glucose levels positions AZD1092 as a critical compound for advancing research in diabetes treatment and management.
Glucolipsin B is a potent glucokinase activator that enhances glucose metabolism by promoting the function of this key enzyme in the glycolytic pathway. This compound exhibits significant biological activity by facilitating insulin secretion from pancreatic beta cells, making it a valuable tool for research focused on diabetes and metabolic disorders. Its ability to modulate glycemic control positions Glucolipsin B as an important reagent in studies aimed at understanding glucose homeostasis and the development of therapeutic strategies for related diseases.
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Glucokinase activator 7 is a potent activator of glucokinase, an enzyme that plays a crucial role in glucose metabolism. By enhancing glucokinase activity, this compound demonstrates significant potential in the research of diabetes and hyperglycemia. Its application extends to studies focused on increasing insulin secretion and improving glucose homeostasis, making it a valuable tool for metabolic research.
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Glucolipsin A is a selective activator of glucokinase, an enzyme that plays a vital role in glucose metabolism. This compound enhances glucose uptake and promotes insulin secretion, making it significant in studies of diabetes and metabolic disorders. It is primarily used in research applications aimed at elucidating the mechanisms of glucokinase regulation and potential therapeutic strategies for glucose homeostasis.
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Glucokinase activator 8 functions as a selective activator of glucokinase, enhancing its enzymatic activity. This compound plays a significant role in glucose metabolism and insulin secretion, making it an important tool for research in diabetes and metabolic disorders. Its ability to modulate glucokinase activity has potential applications in drug development and therapeutic strategies targeting glucose homeostasis.
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Glucokinase Activator 5 primarily targets glucokinase, enhancing its activity and promoting glucose metabolism. This compound has demonstrated potential in improving insulin sensitivity and glycemic control, making it relevant for research into diabetes and metabolic disorders. It serves as a valuable tool for studying the regulatory mechanisms of carbohydrate metabolism and assessing therapeutic strategies for managing hyperglycemia.
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