LCZ960 is an orally active glucokinase (GK) activator. LCZ960 stimulates GK activity in hepatocytes in vitro and stimulates glucose uptake in vivo through hepatic GK activation. LCZ960 lowers blood glucose in mice with diet-induced obesity (DIO). LCZ960 maintains normoglycemia and improves glucose tolerance in DIO mice and rats. LCZ960 stimulates glycogen synthase flux and increases hepatic glycogen turnover in rats. LCZ960 induces increased hepatic glycogen recycling. LCZ960 can be used to study high-fat diet-induced obesity and type 2 diabetes.

AM-2394 is a potent and selective Glucokinase agonist (GKA), which catalyzes the phosphorylation of glucose to glucose-6-phosphate.

TMG-123 (TMG123) is a potent small molecule activator of glucokinase (GK) with EC50 of 0.35 and 0.32 uM for human liver and pancreas GK, respectively.

GKM-001 is a potent, liver-selective small molecule activator of glucokinase (GKA), demonstrates glucose lowering effect without hypoglycemia in normal and type II diabetes mellitus (T2DM).

GKA23 is a potent, small molecule glucokinase (GK) activator with EC50 of 152 nM for glucokinase activation in 5 mM glucose, increases glucose uptake in primary rat hepatocytes with EC50 of 201 nM.

BMS-820132 (BMS 820132) is potent, selective, partial glucokinase (GK) activator with AC50 of 29 nM.

MK-0941 is a novel Glucokinase activator (GKA)

Cadisegliatin (TTP-399) is a potential liver-selective glucokinase (GK) activator for type 2 diabetes and has antihyperglycaemic activity.

Sinogliatin (HMS5552, RO5305552) is a mall molecule glucokinase (GCK; GK) activator.

Glucokinase activator 3 is a potent and full Glucokinase (GK) activator with an AC50 of 38 nM. Glucokinase activator 3 has the potential for the research of type 2 diabetes.

AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC 50 of 4 nM.

IHVR-11029 is a small molecule inhibitor of ER α-glucosidases, with an EC50 of 0.09 μM.

GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 shows significant glucose lowering in high fat fed female rats.

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

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

Ro 28-1675 (Ro 0281675) is a potent allosteric GK activator with a SC1.5 value of 0.24± 0.0019 uM.