sulfonylurea

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

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

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

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

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.

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

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

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.

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

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

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.

4-Hydroxytolbutamide is a sulfonylurea and drug metabolite derived from the metabolism of Tolbutamide by CYP2C8 and CYP2C9 Tolbutamide (HLS 831) is a sulfonylurea hypoglycemic agent.

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.

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

Thiohexamide is a first-generation sulfonylurea compound containing a cyclohexyl group, which possesses blood sugar-lowering activity.

Flucetosulfuron is a sulfonylurea herbicide

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

LY 181984 is an sulfonylurea with antitumor properties.

Glycolamide is a sulfonylurea compound containing cyclohexyl groups.

rac-trans-4-hydroxy Glyburide, an active metabolite of the SUR1 Kir6.2 sulfonylurea inhibitor glyburide, is formed by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP2C9. It inhibits glyburide binding to rat brain synaptosomes at high and low affinity sites of SUR1 Kir6.2 with IC50 values of 0.95 and 100 nM, respectively.

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)

trans-Hydroxy Glimepiride is an active metabolite of the sulfonylurea glimepiride, formed primarily in the liver by the cytochrome P450 (CYP) isoform CYP2C9.

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)

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