sulfonylurea

Bensulfuron-methyl (F 5384) is a broad-spectrum herbicide for broadleaf weeds in paddy fields.

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

Gliquidone (AR-DF 26) is a potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.

Glimepiride (HOE-490) is a long-acting, third-generation sulfonylurea with hypoglycemic activity.

trans-hydroxy Glimepiride is an active metabolite of the sulfonylurea glimepiride .1It is formed from glimepiride primarily in the liver by the cytochrome P450 (CYP) isoform CYP2C9. 1.Langtry, H.D., and Balfour, J.A.Glimepiride. A review of its use in the management of type 2 diabetes mellitusDrugs55(4)563-584(1998)

Carbutamide is a sulfonylurea antidiabetic agent with hypoglycemic activity.

trans-carboxy Glimepiride is a metabolite of the sulfonylurea glimepiride .1It is formed from glimepiride in a two-step process mediated by the cytochrome P450 (CYP) isoform CYP2C9 and cytosolic enzymes. 1.Noh, K., Kim, E., Jeong, T.C., et al.Simultaneous determination of glimepiride and its metabolites in human plasma by liquid chromatography coupled to a tandem mass spectrometryArch. Pharm. Res.34(12)2073-2078(2011)

Glycolamide is a sulfonylurea compound containing cyclohexyl groups.

rac-trans-4-hydroxy Glyburide is an active metabolite of the SUR1/Kir6.2 sulfonylurea inhibitor glyburide .1,2It is formed from glyburide by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9.1rac-trans-4-hydroxy Glyburide inhibits glyburide binding to rat brain synaptosomes at the high and low affinity sites of SUR1/Kir6.2 with IC50values of 0.95 and 100 nM, respectively.2 1.Zharikova, O.L., Fokina, V.M., Nanovskaya, T.N., et al.Identification of the major human hepatic and placental enzymes responsible for the biotransformation of glyburideBiochem. Pharmacol.78(12)1483-1490(2009) 2.Hill, R.A., Rudra, S., Peng, B., et al.Hydroxyl-substituted sulfonylureas as potent inhibitors of specific [3H]glyburide binding to rat brain synaptosomesBioorg. Med. Chem.11(9)2099-2113(2003)

Guanosine 5’-diphosphate (GDP) is a purine nucleotide and biosynthetic precursor of guanosine 5’-triphosphate .1It has been used to study the conformations of GTPases.2GDP (100 μM) activates sulfonylurea receptor 2B (SUR2B) linked to the inward-rectifier potassium channel 6.1 (Kir6.1) in HEK293T cells in a patch-clamp assay.3 1.Berg, J.M., Tymoczko, J.L., and Stryer, L.Biochemistry(2002) 2.Vetter, I.R., and Wittinghofer, A.The guanine nucleotide-binding switch in three dimensionsScience294(5545)1299-1304(2001) 3.Yamada, M., Isomoto, S., Matsumoto, S., et al.Sulphonylurea receptor 2B and Kir6.1 form a sulphonylurea-sensitive but ATP-insensitive K+ channelJ. Physiol.499(Pt 3)715-720(1997)

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

Foramsulfuron, a postemergence sulfonylurea herbicide, selectively controls grass and certain broadleaved weeds in maize (Zea mays L.). It targets acetolactate synthase (ALS), an essential enzyme in the biosynthesis of branched chain amino acids, thus inhibiting weed growth [1].

4-Hydroxytolbutamide(Hydroxytolbutamide), a metabolite of Tolbutamide, which is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic[1][2].

Tribenuron, a slow acting sulfonylurea herbicide, controls broadleaf weed.

Flucetosulfuron is a sulfonylurea herbicide

INF200 (compound 5), a sulfonylurea-based inhibitor of NLRP3 and associated pyroptosis, exhibits cardiometabolic benefits in a rat model of high-fat diet (HFD)-induced metaflammation and demonstrates anti-inflammatory effects by reducing IL-1β release in human macrophages at a concentration of 10 μM. Additionally, it enhances glucose and lipid profiles, diminishes systemic inflammation and cardiac dysfunction biomarkers, notably BNP, and ameliorates myocardial damage linked to ischemia/reperfusion injury (IRI) as assessed by hemodynamic parameters [1].

Anticancer agent 34 (compound 9) is a sulfonylurea derivative and a potent anti-microbial and anti-cancer agent. anticancer agent 34 showed inhibition of microbial growth of Mycobacterium, Escherichia coli and Candida albicans (MIC: 0.039-0.156 mg/ml). Anticancer agent 34 inhibited the growth of A549 cells (IC50: 8.4 μg/ml), PC3 cells (IC50: 7.8 μg/ml).

Acetohexamide (Acetohexamid) is an intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. It inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2) with Ki values of 22.9 and 14.2 μM in HEK293 cells transfected with the human receptor and in rat brain, respectively. Acetohexamide is metabolized in the liver to its active metabolite hydroxyhexamide.

Gliclazide-d7 is a deuterated compound of Gliclazide. Gliclazide has a CAS number of 21187-98-4. Gliclazide, an oral antihyperglycemic agent, belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating beta-cells of the pancreas to release insulin.

Metsulfuron-methyl is a systemic selective wheat field high-efficiency sulfonylurea herbicide, which mainly controls most broadleaf weeds and grass weeds in wheat fields.

Emlenoflast sodium (MCC7840 sodium), a sulfonylurea, is a selective NLRP3 inflammasome inhibitor with an IC50 value of less than 100 nM for NLRP3 inflammasome, and can be used in the study of inflammatory diseases.

Emlenoflast (MCC7840) is a selective inhibitor of NLRP3 inflammasome.

Anticancer agent 35 (compound 10), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 35 inhibits A549, A431, PACA2 cell growth with IC 50 s of 18.1 μg/mL, 4.0 μg/mL, 18.9 μg/mL, respectively [1].

Glieptide, a second-generation sulfonylurea, promotes the accumulation of fructose 2, 6-diphosphate in liver cells.

Anticancer agent 36 (compound 11) is a potent anti-microbial and anti-cancer agent, a sulfonylurea derivative. anticancer agent 36 inhibits the microbial growth of Bacillus mycoides, Escherichia coli and Candida albicans (MIC: 0.156 - 0.039 mg/mL). Anticancer agent 36 inhibited the growth of A549 cells (IC50: 19.7 μg/mL), PC3 cells (IC50: 11.9 μg/mL).

Nicorandil-d4 is intended for use as an internal standard for the quantification of nicorandil by GC- or LC-MS. Nicorandil is an activator of sulfonylurea receptor 2B (SUR2B) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = ~10 µM) and a nitric oxide (NO) donor. It is selective for SUR2B/Kir6.2 over the SUR2A/Kir6.2 channel (EC50 = >500 µM). Nicorandil activates soluble guanylate cyclase in a cell-free assay and relaxes partially depolarized isolated bovine coronary artery strips (EC50 = 4.4 µM). It decreases mean blood pressure, coronary resistance, and heart rate, as well as increases coronary sinus outflow, in dogs when administered intravenously at a dose of 1 mg/kg. Nicorandil increases survival and decreases infarct size in a rabbit model of myocardial ischemia-reperfusion injury induced by left coronary artery occlusion. Formulations containing nicorandil have been used in the treatment of angina pectoris.

Nicorandil N-oxide, a metabolite of nicorandil, functions as an activator of the ATP-sensitive potassium channel Kir6.2 (SUR2B/Kir6.2) and is associated with the sulfonylurea receptor 2B (SUR2B), while also serving as a nitric oxide donor.

P-1075 opens mitochondrial K(ATP) channels and generates reactive oxygen species causing cardioprotection of rabbit hearts. P-1075 is an effective activator of sulfonylurea receptor 2-associated ATP-sensitive potassium channels (SUR2-KIR6) (EC50: 45 nM fo

LY 181984 is an sulfonylurea with antitumor properties.

Glyparamide is a chlorophenyl-containing sulfonylurea with hypoglycemic activity.

Torsemide (AC-4464) is an anilinopyridine sulfonylurea belonging to the class of loop diuretics. Torsemide has a prolonged duration of action compared to other loop diuretics, is extensively protein bound in plasma and has a relatively long half-life.

Rimsulfuron (DPX-E9636) is a sulfonylurea herbicide specifically designed for postemergence application in maize crops. This compound effectively targets and manages grasses as well as certain types of broadleaf weeds.

Anticancer agent 37 (compound 18) is a sulfonylurea derivative known for its potent anticancer activity. It efficiently inhibits the growth of HePG2 cells, displaying an IC 50 value of 17.2 μg/mL [1].

Gliquidone sodium is a hypoglycemic sulfonylurea which may protect the liver from injury from diabetes.

Gliclazide-d4 is intended for use as an internal standard for the quantification of gliclazide by GC- or LC-MS. Gliclazide is a sulfonylurea and an inhibitor of pancreatic β-cell ATP-sensitive potassium (KATP) channels. It is selective for pancreatic β-cell over cardiac and arterial smooth muscle cell KATP channels. Gliclazide (5 μM) increases insulin-induced glucose uptake and glucose transporter 4 (GLUT4) translocation to the plasma membrane in a differentiated 3T3L1 adipocyte model of insulin resistance induced by hydrogen peroxide. Gliclazide (5 and 10 μg/ml) reduces LDL oxidation by human aortic smooth muscle cells (HASMCs), decreasing TBARS content and 8-isoprostane levels. It also decreases oxidized LDL-induced HASMC proliferation and monocyte adhesion when used at concentrations ranging from 1 to 10 μg/ml. Gliclazide (5 mg/kg) reduces serum glucose levels and increases glucose uptake by isolated rat hindquarters in a model of diabetes induced by streptozotocin (STZ).

Thifensulfuron-methyl (Pinnacle) is a sulfonylurea (SU) herbicide, has an important role in the removal of broadleaf weeds.

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

Gliclazide (SE1702), an oral antihyperglycemic agent, belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating beta-cells of the pancreas to release insulin.

Glimepiride urethane is a third generation sulfonylurea compound, which increases the release of insulin from pancreatic beta cells. In addition, glimepiride increases the activity of intracellular insulin receptors. Glimepiride increases osteoblast proliferation and differentiation, which is thought to be related to its ability to activate the PI3K and Akt pathway. Furthermore, Glimepiride enhances intrinsic peroxisome proliferator-activated receptor γ activity. Glimepiride also increases protein expression of glucose transports 1 and 4, and is a potent KIR channel blocker.

Nicosulfuron (Milagro) is a pesticide that works by inhibiting the acetolactate synthase enzyme. Nicosulfuron has not been found to induce mutagenic or carcinogenic effects. Nicosulfuron is a herbicide to protect corn crops from weeds.

Glipizide-d11 is a deuterated compound of Glipizide. Glipizide has a CAS number of 29094-61-9. Glipizide is a short-acting, second-generation sulfonylurea with hypoglycemic activity.

Gliquidone-d6 is a deuterated compound of Gliquidone. Gliquidone has a CAS number of 33342-05-1. Gliquidone is a potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.