Gliclazide
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| Category | Antidiabetic |
| Catalog number | BBF-05867 |
| CAS | 21187-98-4 |
| Molecular Weight | 323.41 |
| Molecular Formula | C15H21N3O3S |
| Purity | >98% |
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Description
Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
Specification
| Synonyms | Gliclazide; Diamicron; Glimicron; Nordialex; Diaikron; S-1702; S-852; S1702; S852; S 1702; S 852 |
| Storage | Store at -20°C |
| IUPAC Name | 1-(3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-2-yl)-3-(4-methylphenyl)sulfonylurea |
| Canonical SMILES | CC1=CC=C(C=C1)S(=O)(=O)NC(=O)NN2CC3CCCC3C2 |
| InChI | InChI=1S/C15H21N3O3S/c1-11-5-7-14(8-6-11)22(20,21)17-15(19)16-18-9-12-3-2-4-13(12)10-18/h5-8,12-13H,2-4,9-10H2,1H3,(H2,16,17,19) |
| InChI Key | BOVGTQGAOIONJV-UHFFFAOYSA-N |
Properties
| Appearance | White crystalline powder |
| Application | Hypoglycemic Agents |
| Melting Point | 160-166°C |
| Density | 1.4±0.1 g/cm3 |
| Solubility | Soluble in Chloroform (Slightly), Methanol (Slightly) |
| LogP | 3.43030 |
Reference Reading
1.A dizygotic twin pregnancy in a MODY 3-affected woman.
Bitterman O1, Iafusco D2, Torcia F3, Tinto N4, Napoli A5. Acta Diabetol. 2016 Mar 21. [Epub ahead of print]
BACKGROUND: MODY diabetes includes rare familiar forms due to genetic mutations resulting in β-cell dysfunction. MODY 3 is due to mutations in the gene transcription factor HNF-1α, with diabetes diagnosis in adolescence or early adult life. Few data are available about MODY 3 in pregnancy.
2.[Risk and benefit of sulfonylureas--their role in view of new treatment options for type 2 diabetes].
Rustenbeck I. Med Monatsschr Pharm. 2016 Feb;39(2):65-72; quiz 73-4.
Currently, the therapy with oral antidiabetic drugs undergoes major changes. The use of sulfonylureas is in marked decline. The major argument in favor of newer oral antidiabetic drugs is the lower risk of hypoglycemia. At the present time however, it is unclear whether DDP4 inhibitors or SGLT2 inhibitors lead to better outcomes with respect to cardiovascular events and overall mortality. Most evidence on the therapeutic use of sulfonylureas has been gained with glibenclamide and to some degree sulfonylureas and glibenclamide have become synonymous. Since sulfonylureas vary considerably in their affinity for the K(ATP) channel subtypes and in their pharmacokinetic properties, the epidemiological evidence that outcomes tend to be less favorable with glibenclamide than with glimepiride or gliclazide has gained some attention. Beyond debate is the efficacy of metformin to diminish cardiovascular events in type 2 diabetes, probably due to effects beyond the lowering of blood glucose.
3.Dose-response relationship between sulfonylureas and major adverse cardiovascular events in elderly patients with type 2 diabetes.
Abdelmoneim AS1,2, Eurich DT2,3, Senthilselvan A3, Qiu W2, Simpson SH1,2. Pharmacoepidemiol Drug Saf. 2016 Apr 22. doi: 10.1002/pds.4014. [Epub ahead of print]
PURPOSE: The objective of this study was to determine if there is a dose-response relationship between sulfonylureas and major adverse cardiovascular events (MACE).
4.Zero-order controlled delivery of Gliclazide from polyethylene oxides matrix tables: In vitro and in vivo evaluation.
Wang L, Yang X1, Di Y, Chen K, Wen H, Pan W. Curr Drug Deliv. 2016 Mar 22. [Epub ahead of print]
BACKGROUND: In recent years, controlled and sustained release drug delivery system has become the focus of pharmaceutical researchers. Some technologies aimed to develop the controlled and sustained release of the drug, which used to be administered several times a day and generate plasma concentration fluctuation. As all, a controlled drug release rate has always been a goal pursued by researchers. This paper introduced a controlled delivery hydrophilic matrix system, and evaluated their relevance between in vitro and in vivo behaviors.
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Bio Calculators
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳
