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K+ channel blocker
BML-KC120-0005 5 g 56.00 USD
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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 Specification

Alternative Name:Glibenclamide
MI:14: 4478
Purity:≥98% (Assay)
Appearance:White to off-white solid.
Solubility:Soluble in DMSO (25mg/ml) or 100% ethanol (5mg/ml).
Long Term Storage:Ambient
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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Product Literature References

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;
D.R. Gehlert, et al.; J. Pharmacol. Exp. Ther. 257, 901 (1991), 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;
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; Full Text
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;

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