GRA Ex-25 is an orally active human glucagon receptor antagonist in a transgenic murine pharmacodynamic model at 10 and 30 mpk.

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively.

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

MK-3102 (MSD) is a novel DPP-4 Inhibitor, which improves glycaemic control with low risk of symptomatic hypoglycaemia.

Bexagliflozin is a potent and selective SGLT2 inhibitor with IC50 value of 5.6 μM /2 nM in SGLT1 /SGLT2 respectively.

Teglicar, in vitro and in animal models, reduces gluconeogenesis and improves glucose homeostasis, refreshing the interest in selective and reversible L-CPT1 inhibition as a potential antihyperglycemic approach.

BVT 14225 is a new selective 11b-HSD1 inhibitor, it belongs to a class of arylsulfonamidothiazoles with in vitro and in vivo antidiabetic effects

Epalrestat is an orally active aldose reductase inhibitor that acts on diabetic neuropathy.

Dapagliflozin, also known as BMS-512148, is a drug used to treat type 2 diabetes approved in 2012 by FDA. Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2) which are responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter mechanism causes blood glucose to be eliminated through the urine. In clinical trials, dapagliflozin lowered HbA1c by 0.6 versus placebo percentage points when added to metformin.

HSD-016 (HSD016) is a potent, selective, and efficacious 11β-HSD1 inhibitor with IC50 of 149 and 530 nM for mouse and human 11β-HSD1, respectively.

ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively.

INCB13739 (INCB-13739) is a potent, selective, oral 11βHSD1 inhibitor (IC50=1.1 nM) with high seelctivity over other dehydrogenases, glucocorticoid and mineralocorticoid receptors..

TAK-875 is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 0.072 μM.

Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.

PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.

PF-04971729 is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2, is currently in phase 2 trials for the treatment of diabetes mellitus.

O304 is a novel AMPK activator.

MK-8722 is a systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.

MK-8245 is an liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.

MK-0941 is a novel Glucokinase activator (GKA)

LX-4211 is a potent dual SGLT2/1 inhibitor; Antidiabetic agents.

GKT137831 is a novel and specific dual Nox1/Nox4 inhibitor with Ki of 140±40 nM and 110±30 nM; a potent inhibitor of fibrosis and hepatocyte apoptosis.

CAY10415 is a potent, antidiabetic drug of the TZD structural class.

Canagliflozin is a highly potent and selective SGLT2 inhibitor for CHO-hSGLT2, CHO-rSGLT2 and CHO-mSGLT2 with IC50 of 4.4 nM, 3.7 nM and 2 nM, respectively.

BVT 2733 is a selective 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor,protecting osteoblasts against endogenous glucocorticoid induced dysfunction.

A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, little effect on GPPase/FBPase activity.

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

Succinobucol is a phenolic antioxidant with anti-inflammatory and antiplatelet effects.

Ipragliflozin (ASP1941) is a Novel Selective Sodium-Dependent Glucose Co-Transporter 2 Inhibitor, on Urinary Glucose Excretion in Healthy Subjects