diabetes mellitus

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

Dapagliflozin (BMS-512148) is a selective sodium-glucose co-transporter subtype 2 (SGLT2) inhibitor with antihyperglycemic activity.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Dapagliflozin ((2S)-1,2-propanediol, hydrate) (BMS-512148 (2S)-1,2-propanediol, hydrate) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2), in development for treating type 2 diabetes mellitus (T2DM). It inhibits SGLT2, responsible for at least 90% of glucose reabsorption in the kidney.

Canagliflozin (JNJ 28431754AAA) is a selective SGLT2 inhibitor that inhibits CHO cells expressing mSGLT2, rSGLT2, and hSGLT2 (IC50=2 3.7 4.4 nM). Canagliflozin can be used for the treatment of type II diabetes mellitus (T2DM).

Anagliptin (SK-0403) is a potent inhibitor of DPP-4 (IC50 of 3.8 nM) used in the treatment of type 2 diabetes mellitus.

Ipragliflozin (ASP1941) is under investigation in Type 2 Diabetes and Diabetes Mellitus, Type 2.

1-Deoxynojirimycin (Moranoline) is a potent α-glucosidase inhibitor, suppressing postprandial blood glucose, thereby possibly preventing diabetes mellitus.

Aegeline is an alkaloidal-amide, isolated from the leaves of Aegle marmelos and have shown antihyperglycemic as well as antidyslipidemic activities in the validated animal models of type 2 diabetes mellitus.

Acarbose (BAY g 5421) is an inhibitor of α-Glucosidases with antihyperglycemic activity.

1. L-Arginine (L-Arg) exhibits anti-atherosclerotic effect. 2. L-Arginine and soy enriched diet are effective in prevention of osteoporosis associated with diabetes mellitus. 3. Exogenous L-Arginine could enhance neonate lymphocyte proliferation through an interleukin-2-independent pathway. 4. A combination of oral L-citrulline and L-Arginine effectively and rapidly augments NO-dependent responses at the acute stage.

Chlorpropamide (Diabinese) is a sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification.

Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein/enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.

Repaglinide (AG-EE 623ZW) is a benzoic acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Repaglinide has been linked to rare instances of clinically apparent acute liver injury.

Glipizide (CP 28720) is a short-acting, second-generation sulfonylurea with hypoglycemic activity.

Deferoxamine Mesylate (DFOM) is an iron chelator and ferroptosis inhibitor. Deferoxamine Mesylate binds free iron into a stable complex and reduces iron accumulation. Deferoxamine Mesylate up-regulates HIF-1α levels and induces apoptosis.

Duloxetine hydrochloride ((S)-Duloxetine hydrochloride) is a thiophene derivative and selective neurotransmitter uptake inhibitor for serotonin and noradrenaline (SNRI). It is an antidepressant agent and anxiolytic, also used for treating pain in patients with diabetes mellitus and fibromyalgia.

Granotapide is a microsomal triglyceride transfer protein (MTP) inhibitor that treats and rather prevents atherosclerosis, coronary artery disease, metabolic syndrome, obesity, diabetes mellitus, prediabetes mellitus, and hypertension.

Lobeglitazone Sulfate（CKD-501 Sulfate） is a novel thiazolidinedione with anti-inflammatory activity that inhibits LPS-induced NLRP3 inflammasome activation and hepatic inflammation, and can be used in the study of type 2 diabetes mellitus (T2DM).

Albiglutide TFA (782500-75-8 free base) (Albiglutide TFA) is a long acting GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus (T2DM).

(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide is an Apelin receptor agonist with an EC50 for Apelin receptors of 0.012 µM.(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5- methylpyrimidin-2-yl)butane-2-sulfonamide is used in the treatment of heart failure, atherosclerosis, obesity, diabetes mellitus, amyotrophic lateral sclerosis, coronary artery disease, hypertension, stroke and myocardial infarction.

Glycogen phosphorylase-IN-1 is a selective and potent inhibitor of human hepatic glycogen phosphorylase (hlGPa) with inhibitory effects on hlGPa activity and on hepatocyte glycogen-derived glucose production, and can be used in the study of type 2 diabetes mellitus and canine lupus.

Globalagliatin (LY2608204) has been used in trials studying the treatment of Diabetes Mellitus, Type 2.

Enpp-1-IN-16 is an inhibitor targeting ENPP1 with potential anti-cancer activity.Enpp-1-IN-16 can be used to study insulin resistance in relation to type II diabetes mellitus and various ENPP1-mediated diseases in the chondrocalcinosis and osteoarthritis classes.

Ciamexon (Ciamexone) is a novel immunomodulator that has shown promising results in experimental models of autoimmune disease with little demonstrated cytotoxicity.Ciamexon can be used to study endocrine ophthalmopathies and diabetes mellitus, with slight improvement in ophthalmic disease following short-term administration.

PF-04937319 is an activator of glucokinase (EC50 =154.4  μM). PF-04937319 maintains glucose-lowering efficacy while mitigating the risk of hypoglycemia observed with many other glucokinase activators. PF-04937319 can be used in research on the treatment of type 2 diabetes mellitus.

K-111 (BM-170744) is an orally available peroxisome proliferator-activated receptor (PPAR)-alpha agonist and insulin enhancer for the study of obesity-type diabetes mellitus and the metabolic syndrome.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

Omarigliptin (MK-3102) has been used in trials studying the treatment of Type 2 Diabetes Mellitus and Chronic Renal Insufficiency.

GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.

AMG131 (CHS 131) , is a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR)gamma modulator, which can be used for the treatment of type 2 diabetes mellitus (non-insulin dependent diabetes)

Chembridge-5861528 (TCS 5861528) is a TRPA1 channel blocker that inhibits AITC- and 4-HNE-induced calcium influx with IC50 values of 14.3 μM and 18.7 μM, respectively.

Isookanin shows strong diphenyl(2,4,6-trinitrophenyl)iminoazanium (DPPH) radical-scavenging activity with the IC50 value of 7.9 ± 0.53 μM. Isookanin is a potent inhibitor of α-amylase (IC50=0.447 mg ml).

AZD9977 is a novel, selective modulator of mineralocorticoid receptor .

YM-440 is a novel hypoglycemic agent, an insulin sensitizer, that may be used for the treatment of type 2 diabetes mellitus by reducing glucose 6-phosphatase activity in obese Zucker rats and inhibiting liver glucose output through gluconeogenesis.

GSK256073 is an agonist of G-protein coupled receptor 109A (GPR109A). It acts by reducing serum glucose in subjects with type 2 diabetes mellitus.

Deanol aceglumate is combination of deanol and N-acetyl-L-glutamic acid. deanol aceglumate can effect Hepatoprotective on stress-induced gastropathy and diabetes mellitus.

Mk-0533 is a selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus.

ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesses good in vitro drug-like properties (aqueous solubility, cell permeability, low low potential for drug-drug interactions, low predicted hepatic clearance), and selectivity against broad panels of receptors and enzymes.

α-Glucosidase-IN-26 (Compound 7i), with an IC50 value of 4.63 µM, functions as an α-glucosidase inhibitor and is utilized in type 2 diabetes mellitus (T2DM) research [1].

INCB13739 is an orally active, potent, selective, and tissue-specific inhibitor of 11β-HSD1 (11β-hydroxysteroid dehydrogenase 1), with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC). It is used in research for type 2 diabetes mellitus (T2DM) and obesity [1].

Piragliatin, also known as RO4389620, is a glucokinase activator. Piragliatin greatly enhances glucose-induced pancreatic islet respiration and insulin release. Piragliatin lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus. Piragliatin has an acute glucose-lowering action in patients with mild type 2 diabetes, mainly mediated through a generalized enhancement of β-cell function and through fasting restricted changes in glucose turnover.

Saxagliptin is a new oral hypoglycemic of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones and reducing fasting and postprandial glucose conce

VULM 1457 is a potent ACAT inhibitor. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells.

Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC), a potent inhibitor of 12 15-Lipoxygenases (LO), shows potential in type 1 diabetes mellitus research [1].

Dutogliptin (PHX-1149 free base) is an effective, selective oral dipeptidyl peptidase-4 (DPP4) inhibitor used for treating type 2 diabetes mellitus.

GAD65 (206-220) is a synthetic peptide derived from glutamic acid decarboxylase (GAD) 65, specifically corresponding to residues 180-188. It is known that GAD65 interacts with I-Ag7 MHC class II molecules and is a significant pancreatic antigen that self-reactive T cells target in type I diabetes mellitus.

Diacerein (Fisiodar) is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including sevre diarrhea [L780]. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.

γ-Glu-Tyr (gamma-Glutamyltyrosine) is a kokumi peptide with competitive inhibition of dipeptidyl peptidase-IV (DPP-IV) and is used in the study of diabetes mellitus.

Wy 41747 is a long-acting somatostatin analogue used in diabetes mellitus research [1].