store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Glibenclamide [10238-21-8]
Référence T1634-1g
Conditionnement : 1g
Marque : TargetMol
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Glibenclamide
Catalog No. T1634 CAS 10238-21-8
Synonyms: Glyburide
Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide.
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Glibenclamide, CAS 10238-21-8
| Description | Glibenclamide (Glyburide) is an antidiabetic sulfonylurea derivative with actions similar to those of chlorpropamide. |
| In vitro | Administered intravenously at a dose of 25 mg/kg, Glyburide increased sodium (Na) ion excretion by 350% one hour after treatment, without affecting potassium (K) ion excretion, glomerular filtration rate, mean arterial pressure, or heart rate. In awake rats subjected to a saline load, Glyburide dose-dependently increased urinary sodium excretion, while urinary potassium excretion remained largely unchanged. |
| In vivo | Glyburide enhances the apparent affinity of scavenger receptor class B type I (SR-BI) for high-density lipoprotein (HDL) binding in insulin-secreting cells. It inhibits SR-BI-mediated selective lipid uptake and efflux, with potency similar to its inhibition of ABCA1 (IC50 approximately 275-300 mM). Regardless of the pre-existing relaxation level, Glyburide can also reverse the relaxation induced by pinacidil. At a concentration of 0.03 mM, Glyburide blocks ATP-modulated potassium channels in insulin-secreting cells. It causes a concentration-dependent increase in the IC50 values for BRL34915 and diazoxide, eliminating the relaxation response to minoxidil sulfate. Doses of Glyburide ranging from 10-500 nM proportionately inhibit the relaxation time brought about by potassium channel openers. |
| Synonyms | Glyburide |
| Molecular Weight | 494 |
| Formula | C23H28ClN3O5S |
| CAS No. | 10238-21-8 |
Storage
Solubility Information
DMSO: 99 mg/mL (200.4 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
References and Literature
1. Winquist RJ, et al. J Pharmacol Exp Ther,1989, 248(1), 149-156. 2. Nieland TJ, et al. J Lipid Res,2004, 45(7), 1256-1265. 3. Brady PA, et al. Eur J Pharmacol,1996, 308(3), 343-349. 4. Meisheri KD, et al. J Vasc Res,1993, 30(1), 2-12. 5. Clark MA, et al. J Pharmacol Exp Ther,1993, 265(2), 933-937. 6. Juarez-Mercado K E, Prieto-Martinez F D, Sanchez-Cruz N, et al. DNA Methyltransferase Inhibitors with Novel Chemical Scaffolds[J]. bioRxiv. 2020 7. Chen F, Xu Y, Wang J, et al. Relaxation Effect of Patchouli Alcohol in Rat Corpus Cavernous and Its Underlying Mechanisms[J]. Evidence-Based Complementary and Alternative Medicine. 2020, 2020. 8. Capoci I R G, Faria D R, Sakita K M, et al. Repurposing approach identifies new treatment options for invasive fungal disease[J]. Bioorganic chemistry. 2019 Mar;84:87-97. 9. Juárez-Mercado K E, Prieto-Martínez F D, Sánchez-Cruz N, et al. Expanding the Structural Diversity of DNA Methyltransferase Inhibitors[J]. Pharmaceuticals. 2021, 14(1): 17.
Citations
1. Juárez-Mercado K E, Prieto-Martínez F D, Sánchez-Cruz N, et al. Expanding the Structural Diversity of DNA Methyltransferase Inhibitors. Pharmaceuticals. 2021, 14(1): 17. 2. Capoci I R G, Faria D R, Sakita K M, et al. Repurposing approach identifies new treatment options for invasive fungal disease. Bioorganic Chemistry. 2019 Mar;84:87-97 3. Chen F, Xu Y, Wang J, et al. Relaxation Effect of Patchouli Alcohol in Rat Corpus Cavernous and Its Underlying Mechanisms. Evidence-Based Complementary and Alternative Medicine. 2020.