Replaces Prod. #: ALX-550-270
ATP-dependent K+ channel blocker in the pancreas, which in turn causes intracellular Ca2+ levels to rise and for insulin to be secreted. It blocks vascular smooth muscle relaxation produced by KATP channel openers. Antidiabetic. High affinity binding sites have been identified in the cardiovascular system, the CNS, and pancreatic beta cells. It displays a large potency difference in pancreatic tissue (IC50 in the nM range) versus vascular tissue (IC50 in the µM range).
Product Details
Alternative Name: | Glibenclamide |
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Formula: | C23H28ClN3O5S |
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MW: | 494.0 |
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CAS: | 10238-21-8 |
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MI: | 14: 4478 |
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RTECS: | YS4725200 |
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Purity: | ≥98% (Assay) |
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Appearance: | White to off-white solid. |
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Solubility: | Soluble in DMSO (25mg/ml) or 100% ethanol (5mg/ml). |
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Shipping: | Ambient Temperature |
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Long Term Storage: | Ambient |
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Use/Stability: | Stable for at least 1 year after receipt when stored, as supplied, at room temperature. Stock solutions are stable for up to 3 months at -20°C. |
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Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Vasorelaxant and Antioxidant Effects of Aframomum pruinosum Gagnep. (Zingiberaceae) Seed Extracts May Mediate Their Cardioprotective Activity against Isoproterenol-Induced Myocardial Infarction: E.P. Nguelefack-Mbuyo, et al.; Evid. Based Complement. Alternat. Med.
2022, 7257448 (2022),
Abstract;
Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor: K. Ramkumar, et al.; Nat. Commun.
7, 13084 (2016),
Application(s): Western blot, HCT116 cells,
Abstract;
Full Text
Glyburide and tolbutamide induce desensitization of insulin release in rat pancreatic islets by different mechanisms: A.M. Rabuazzo, et al.; Endocrinology
131, 1815 (1992),
Abstract;
High affinity [3H]glibenclamide binding sites in rat neuronal and cardiac tissue: localization and developmental characteristics: J.A. Miller, et al.; J. Pharmacol. Exp. Ther.
256, 358 (1991),
Abstract;
Quantitative autoradiography of the binding sites for [125I] iodoglyburide, a novel high-affinity ligand for ATP-sensitive potassium channels in rat brain: D.R. Gehlert, et al.; J. Pharmacol. Exp. Ther.
257, 901 (1991),
Abstract;
Potassium channel modulators: scientific applications and therapeutic promise: D.W. Robertson & M.I. Steinberg; J. Med. Chem.
33, 1529 (1990),
Abstract;
Glyburide blocks the relaxation response to BRL 34915 (cromakalim), minoxidil sulfate and diazoxide in vascular smooth muscle: R.J. Winquist, et al.; J. Pharmacol. Exp. Ther.
248, 149 (1989),
Abstract;
In vitro effects of sulfonylurea on glucose transport and translocation of glucose transporters in adipocytes from streptozocin-induced diabetic rats: D.R. Jacobs, et al.; Diabetes
38, 205 (1989),
Abstract;
Antidiabetic sulfonylureas control action potential properties in heart cells via high affinity receptors that are linked to ATP-dependent K+ channels: M. Fosset, et al.; J. Biol. Chem.
263, 7933 (1988),
Abstract;
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The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated K+ channel in insulin-secreting cells: H. Schmid-Antomarchi, et al.; J. Biol. Chem.
262, 15840 (1987),
Abstract;
Glyburide: a second-generation sulfonylurea hypoglycemic agent. History, chemistry, metabolism, pharmacokinetics, clinical use and adverse effects: J.M. Feldman; Pharmacotherapy
5, 43 (1985),
Abstract;
Intracellular ATP directly blocks K+ channels in pancreatic B-cells: D.L. Cook & C.N. Hales; Nature
311, 271 (1984),
Abstract;
Glipizide: a review of its pharmacological properties and therapeutic use: R.N. Brogden, et al.; Drugs
18, 329 (1979),
Abstract;