antidiabetic

Compound 56 (Antidiabetic agent 2) is a glucose-uptake promoter that inhibits DPP-4, PTP-1B, α-amylase, and α-glucosidase, with IC50 values of 0.036, 0.042, 0.241, and 0.185 μM, respectively. This agent effectively decreases blood glucose levels [1].

GLP-1(7-36) amide (MKC 253) is a peptide hormone released from intestinal L-cells upon nutrient intake. It binds to the GLP-1 receptor in the pancreas, enhancing insulin secretion from pancreatic β-cells and increasing insulin expression, thereby exhibiting antidiabetic effects.

Imeglimin (EMD 387008) is an orally available antidiabetic compound that enhances mitochondrial function, enhances insulin secretion, promotes β-cell proliferation and improves pancreatic β-cell survival in mice.

Rosiglitazone maleate (BRL 49653) is the maleate salt of rosiglitazone, an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.

Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.

Buformin hydrochloride (NSC-528218) is a potent AMPK activator,an oral antidiabetic drug of the biguanide class. Buformin delays the absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake into cells and inhibits synthesis of glucose by the liver. Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.

Pioglitazone hydrochloride (AD 4833) is the hydrochloride salt of an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Costunolide (Costus lactone) has anti-inflammatory and anti-oxidant properties and mediates apoptosis.

1H-pyrazole (1,2-Diazole), is a versatile building block, with a vast applications in organic synthesis. The derivatives of Pyrazole are used in medicine, for their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, tranquilizing, muscle relaxing, psychoanaleptic, anticonvulsant, monoamineoxidase inhibiting, antidiabetic and antibacterial activities.

Zingerone (Vanillylacetone) is a nontoxic methoxyphenol isolated from Zingiber officinale, with potent anti-inflammatory, antidiabetic, antidiarrhoeic, antilipolytic, antispasmodic, and anti-tumor properties. Zingerone (Gingerone) alleviates oxidative stress and inflammation, down-regulates NF-κB mediated signaling pathways, acts as an anti-mitotic agent, and inhibits the growth of neuroblastoma cells.

LX-4211 intermediate is a synthetic intermediate of LX-4211, a potent SGLT1/2 inhibitor used as an antidiabetic agent.

Dehydrocostuslactone is a natural product extracted from Aucklandia.It has wide spectrum of biological effects, including anti-inflammatory, anticancer, antiviral, antimicrobial, antifungal, antioxidant, antidiabetic, antiulcer, and anthelmintic activitie

TS-021 is a selective dipeptidyl peptidase 4 (DPP-4) inhibitor with antidiabetic activity for the study of type 2 diabetes.

Paeonoside, found in P. suffruticosa, is biologically active and can promote wound healing and migration during osteoblast differentiation. Paeonoside has certain antidiabetic activity and may prevent sepsis and death from sepsis. Paeonoside has no cytotoxic effect on preosteoblasts of MC3T3-E1 cells, significantly restores the wound area and promotes cell migration and alkaline phosphatase (ALP) staining and its activity in a dose-dependent manner.

T-1095 is an inhibitor of renal glucose reabsorption and the expression of Na+-glucose cotransporters (SGLTs) and facilitative glucose transporter 2 (GLUT2).

Darglitazone (CP-86325) is a potent, selective agonist of PPAR-γ with antidiabetic actions. Darglitazone is effective in controlling blood glucose and lipid metabolism.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.

Cichoric Acid (Dicaffeoyltartaric acid) is a potent inhibitor of human immunodeficiency virus type-1 (HIV-1) integrase and the replication in tissues. It also a class of cannabinomimetics with CB2 receptor-dependent and independent.

1. Berberrubine chloride (9-Berberoline Chloride) has antitumor activity. 2. Berberrubine has antidiabetic activity. 3. Berberrubine dose-dependently inhibits IL-8 and MCP-1 protein levels in the media and mRNA expression of the cells stimulated with IL-1beta or TNF-alpha.

(+)-Magnoflorine (Thalictrin) has sedative and anxiolytic effects, probably mediated by Magnoflorine through a GABAergic mechanism of action. Magnoflorine and Sinomenine have protective effects, are mediated by some mechanism other than prevention of micelle formation or protection of the erythrocyte membrane against osmotic imbalance.

1. Eriodictyol (Huazhongilexone) is a flavonoid with anti-inflammatory and antioxidant activities. 2. Eriodictyol may possess antidiabetic properties through increasing glucose uptake and improving insulin resistance. 3. Eriodictyol may be a potential therapeutic resource for Atopic dermatitis and an adjunctive agent to control itchiness inAtopic dermatitis.

MSDC 0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being used in trials studying the treatment of Type 2 Diabetes and Alzheimer's Disease.

D-Tagatose (D-(-)-Tagatose), a rare natural hexoketose and isomer of D-galactose, occurs naturally in Sterculia setigera gum and is found in small quantities in various foods such as sterilized and powdered cow's milk, hot cocoa, and various cheeses, yogurts, and other dairy products. It can be synthesized from D-galactose by isomerization under alkaline conditions in the presence of calcium. D-Tagatose has numerous health benefits, including promotion of weight loss, no glycemic effect, anti-plaque, non-cariogenic, anti-halitosis, prebiotic, and anti-biofilm properties; it is beneficial for organ transplants, enhancement of flavor, improvement of pregnancy and fetal development, treatment of obesity, and reduction in symptoms associated with type 2 diabetes, hyperglycemia, anemia, and hemophilia. (PMID: 17492284).

Glymidine sodium is a sulfonamide hypoglycemic agent which stimulates insulin secretion.

Gossypin has antidiabetic, antioxdiant, anticonvulsant, anti-allergic, antiinflammatory, antinociceptive, cytotoxic and antibacterial activities; it inhibits the NF-kappaB activation pathway, which may explain its role in the suppression of inflammation,

Carbutamide is a sulfonylurea antidiabetic agent with hypoglycemic activity.

Mogroside II-A2 is a natural product from Siraitia grosvenorii Swingle. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.

Sirtuin modulator 2 (N-(3-(imidazo[2,1-b]thiazol-6-yl)phenyl)-2-methoxybenzamide) exhibits antidiabetic, anti-inflammatory and antitumor activities.

VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3, M5 positive allosteric modulator (PAM),and is a neuroprotective agent.

Kaempferol 3-O-gentiobioside, a flavonoid isolated from C. alata leaves, exhibits antidiabetic activity and α-glucosidase inhibition, demonstrating a carbohydrate enzyme inhibitory effect (IC50: 50 μM).

Nepodin has antimalarial, and anti-inflammatory activities, it shows significant cyclooxygenase (COX) inhibitory activity. Nepodin has an antidiabetic effect, which is at least partly mediated by stimulation of GLUT4 translocation via AMPK activation by n

Mogroside IIA1 (Mogroside II-A1) is isolated from the fruits of Siraitia grosvenorii. Mogroside IIA1 is a a nonsugar sweetener and sweeter than sucrose. Mogroside IIA1 possesses antioxidant, antidiabetic and anticancer activities.

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

Bruceine E is isolated from B. javanica seeds with hypoglycemia effects. Bruceine E can be used for studies about acting as an insulin secretagogue.

Mogrosides IV is a sweet minor cucurbitane glycoside, it exhibits maltase inhibitory effect(IC50 : 10 mM), and with antioxidant, antidiabetic and anticancer activities.

GSK-3β inhibitor 1 is an inhibitor of GSK-3β( IC50 of 4.9 nM) and demonstrates high antidiabetic efficacy.

ISOTHIAZOLINE 1,1-DIOXIDE (isothiazolidine 1,1-dioxide) is a reactant used in the synthesis of orally bioavailable hebatits B caspid inhibitors, and in the preparation of cryptochrome imhibitors as antidiabetic agents.

Mifobate (SR-202) is a potent and specific antagonist of PPARγ, exhibiting antiobesity, antidiabetic, and antiatherosclerotic effects[1].

Enavogliflozin (DWP-16001) is an orally available small molecule and sodium glucose transporter 2 inhibitor.

(+)-Magnoflorine chloride (Escholine chloride) has anti-inflammatory activity, it can inhibit inflammations.

MAP4K4-IN-3 (Compound 17), a serine threonine protein kinase, may be a viable target for antidiabetic agents.

Azoramide, a small-molecule modulator, has the antidiabetic activity of unfolded protein response.

Gomisin D is a natural product

(E Z)-GSK-3β inhibitor 1 is a glycogen synthase kinase 3β (GSK-3β) inhibitor demonstrating high antidiabetic efficacy.

Arjunolic acid has antioxidant, anti-inflammatory, antinociceptive and anticholinesterasic (AChE and BuChE) activities, it may as promising targets for the development of innovative multi-functional medicines for Alzheimer desease treatment.

BM-131246 is an orally available and antidiabetic active thiazolidinedione derivative for the study of diabetes.

Ficusonolide exhibits significant antidiabetic activity through its interactions with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase.