356310

Glyburide

A sulfonylurea that selectively blocks ATP-sensitive K⁺ channels.

• Synonyme(s) : Glyburide, Glybenclamide
• Formule empirique (notation de Hill): C₂₃H₂₈ClN₃O₅S
• Numéro CAS: 10238-21-8
• Poids moléculaire : 494.00
• Numéro MDL: MFCD00056625
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (TLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze
• Couleur: white
• Solubilité: DMSO: 25 mg/mL; ethanol: 5 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 10-30°C
• InChI: 1S/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29)
• Clé InChI: ZNNLBTZKUZBEKO-UHFFFAOYSA-N

Description

Description générale

A sulfonylurea that selectively blocks ATP-sensitive K⁺ channels. Reduced K⁺ conductance causes membrane depolarization and influx of Ca²⁺ through voltage sensitive Ca²⁺ channels. Blocks vascular smooth muscle relaxation produced by K_ATP channel openers. Inhibits the vasorelaxing effects of nitric oxide.

Antidiabetic sulfonylurea that selectively blocks ATP-sensitive K⁺ channels. Reduced K⁺ conductance causes membrane depolarization and influx of Ca²⁺ through voltage sensitive Ca²⁺ channels. Blocks vascular smooth muscle relaxation produced by K_ATP channel openers. High-affinity binding sites are widely distributed and have been identified in the cardiovascular system, the central nervous system, and pancreatic β-cells. In cultured cells, glyburide enhances insulin action and stimulates the synthesis of glucose transporters. Displays large potency difference in action on pancreatic tissue (IC₅₀ in nM range) and vascular tissue (IC₅₀ in µM range).

Actions biochimiques/physiologiques

Cell permeable: no

Primary Target
ATP-sensitive K+ channels

Product does not compete with ATP.

Reversible: no

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Holzmann, S., et al. 1992. Eur. J. Pharmacol.215, 1.
Rabuazzo, A.M., et al. 1992. Endocrinology131, 1815.
Miller, J.A., et al. 1991. J. Pharmacol. Exp. Ther.256, 358.
Jacobs, D.R., et al. 1989. Diabetes 38, 205.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Mentions de danger: H413
• Conseils de prudence: P273 - P501
• Classification des risques: Aquatic Chronic 4
• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable