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Technical Data
| Formula | C23H28ClN3O5S |
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| Molecular Weight | 494 | CAS No. | 10238-21-8 | |
| Solubility (25°C)* | In vitro | DMSO | 99 mg/mL (200.4 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes. | |
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| In vitro | Glyburide (0.03 mM), a sulfonylurea which has been shown to block the ATP-modulated potassium channel in insulin-secreting cells, causes concentration-dependent shifts to the right (up to 100-fold) of the IC50 value for BRL 34915 and diazoxide, and at 1 μM, abolishes the relaxation response to minoxidil sulfate. [1] Glyburide increases the apparent affinity of HDL binding to Scavenger receptor class B type I (SR-BI). Glyburide blocks SR-BI-mediated selective lipid uptake and efflux at a potency similar to that for its inhibition of ABCA1 (IC50 approximately 275-300 mM). [2] Glyburide (6 mM) which reduces the opening of KATP channels, aggravates Ca2+ loading only when applied to dinitrophenol-pretreated myocytes but not when applied with dinitrophenol treatment. [3] Glyburide (10-500 nM) produces a dose-dependent inhibition of the potassium channel openers (PCOs) relaxation time course. Glyburide also reverses existing Pinacidil relaxation regardless of the degree of pre-existing relaxation. Glyburideis is able to produce its blockade regardless of the state of K+ channel activation. [4] | |
| In vivo | Glyburide (GLY) dose-dependently increases urinary Na+ excretion with little change in urinary K+ excretion after i.p. administration (10-100 mg/kg) in saline-loaded conscious rats. Glyburide (25 mg/kg i.v.) increases Na+ excretion 350% during the first hour post-treatment without affecting K+ excretion, glomerular filtration rate, mean arterial pressure or heart rate. [5] |
Protocol (from reference)
References
Selleck's Glyburide (Glibenclamide) has been cited by 8 publications
| Interrogating direct NLRP3 engagement and functional inflammasome inhibition using cellular assays [ Cell Chem Biol, 2023, S2451-9456(23)00335-5] | PubMed: 37858335 |
| Determination and pharmacokinetics study of UK-5099 in mouse plasma by LC-MS/MS [ BMC Vet Res, 2022, 18(1):145] | PubMed: 35443692 |
| Aeromonas sobria Induces Proinflammatory Cytokines Production in Mouse Macrophages via Activating NLRP3 Inflammasome Signaling Pathways [ Front Cell Infect Microbiol, 2021, 11:691445] | PubMed: 34513725 |
| Anti-SARS-CoV-2 Activity of Extracellular Vesicle Inhibitors: Screening, Validation, and Combination with Remdesivir [ Biomedicines, 2021, 9(9)1230] | PubMed: 34572416 |
| Extracellular vesicles secreted by Giardia duodenalis regulate host cell innate immunity via TLR2 and NLRP3 inflammasome signaling pathways [ PLoS Negl Trop Dis, 2021, 15(4):e0009304] | PubMed: 33798196 |
| The NLRP3 Inflammasome Regulates Corneal Allograft Rejection Through Enhanced Phosphorylation of STAT3 [ Am J Transplant, 2020, 10.1111/ajt.16071] | PubMed: 32583615 |
| NLRP3 Inflammasome Participates in Host Response to Neospora caninum Infection [ Front Immunol, 2018, 9:1791] | PubMed: 30105037 |
| NLRP3 inflammasome activation in murine macrophages caused by Neospora caninum infection [ Parasit Vectors, 2017, 10(1):266] | PubMed: 28558839 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.