Glucokinase Activator

Palmitelaidic acid (9-trans-Hexadecenoic acid) is the trans isomer of palmitoleic acid. Palmitoleic acid is one of the most abundant fatty acids in serum and tissue.

Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes.

GKA50 is a potent glucokinase activator (EC₅₀=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca²⁺-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats.

Globalagliatin (LY2608204) is an orally active glucokinase (GK) activator with an EC₅₀ of 42 nM. Globalagliatin also stimulates glucose metabolism in rat insulinoma INS1-E cells with an EC₅₀ of 579 nM. Globalagliatin targets both pancreatic β-cells and hepatocytes. Globalagliatin is promising for research of type 2 diabetes.

RO-28-1675 is a potent allosteric glucokinase (GK) activator with an EC₅₀ of 54 nM. RO-28-1675 can be used for the research of type 2 diabetes.

MK-0941 is a selective, 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 activates hexokinase subtype IV. MK-0941 can increase insulin secretion and glucose uptake. MK-0941 can be studied in research for type 2 diabetes.

PF-04991532 is a potent, hepatoselective glucokinase activator with EC₅₀s of 80 and 100 nM in human and rat, respectively.

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.

Cadisegliatin (TTP-399) is a potential, orally active liver-selective glucokinase (GK) activator. Cadisegliatin has antihyperglycaemic activity. Cadisegliatin can be used for the research of type 2 diabetes.

Nerigliatin (PF-04937319) is a orally active glucokinase activator (GKA) with EC₅₀ value of 154.4 μM. Nerigliatin maintains glucose-lowering efficacy. Nerigliatin causes peripheral nerve degeneration. Nerigliatin can be used in type 2 diabetes research.

AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC₅₀ of 60 nM.

BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC₅₀ of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation.

AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC₅₀ of 42 nM. AR453588 shows anti-hyperglycemic activity.

Palmitelaidic acid-d₁₃ is the deuterium labeled Palmitelaidic Acid. Palmitelaidic Acid (9-trans-Hexadecenoic acid) is the trans isomer of palmitoleic acid. Palmitoleic acid is one of the most abundant fatty acids in serum and tissue.

GKA50 quarterhydrate is a potent glucokinase activator (EC₅₀=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca²⁺-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats.

Glucokinase activator 3 is an orally active Glucokinase (GK) activator with an AC₅₀ of 38 nM. Glucokinase activator 3 inhibits hERG channel and sodium channel in patch clamp assays. Glucokinase activator 3 exhibits high efficacy in reducing blood glucose in diet-induced obese (DIO) mice. Glucokinase activator 3 has the potential for the research of type 2 diabetes.

Dorzagliatin (Standard) is the analytical standard of Dorzagliatin. This product is intended for research and analytical applications. Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes.

MK-0941 free base is an orally active 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 free base exhibits strong glucose-lowering activity and is a potential therapeutic agent for treatment of type 2 diabetes.

AR453588 hydrochloride is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC₅₀ of 42 nM. AR453588 hydrochloride shows anti-hyperglycemic activity.

Glucokinase activator 1 is a liver-directed glucokinase activator with an EC₅₀ of 34 nM.