Glibenclamide
Based on 28 publication(s) in Google Scholar
Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 10238-21-8
- Formula: C23H28ClN3O5S
- Molecular Weight:494.00
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Glibenclamide
More- Nat Metab. 2022 Feb;4(2):269-283. [Abstract]
- Nat Commun. 2025 Jan 31;16(1):1212. [Abstract]
- Pharmacol Res. 2020 Mar;153:104679. [Abstract]
- Int J Biol Macromol. 2024 Sep 23:135876. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Br J Pharmacol. 2020 May;177(10):2286-2302. [Abstract]
- Cell Rep. 2026 Jun 25;45(7):117613. [Abstract]
- Int J Nanomedicine. 2025 Apr 5:20:4145-4163. [Abstract]
- Virulence. 2022 Dec;13(1):1486-1501. [Abstract]
- Pharmaceuticals (Basel). 2025 Sep 21;18(9):1420. [Abstract]
- Front Pharmacol. 2021 Apr 26:12:641829. [Abstract]
- Eur J Pharmacol. 2025 May 23:177765. [Abstract]
- Int Immunopharmacol. 2024 Oct 27;143(Pt 2):113494. [Abstract]
- BMC Biol. 2021 Mar 3;19(1):40. [Abstract]
- Cancers (Basel). 2023 Jun 3;15(11):3043. [Abstract]
- Front Cell Dev Biol. 2020 May 12;8:269. [Abstract]
- J Cell Physiol. 2024 Feb;239(2):e31117. [Abstract]
- J Periodontal Res. 2022 Jun;57(3):448-460. [Abstract]
- Front Physiol. 2021 Oct 28;12:770430. [Abstract]
- eNeuro. 2022 Jul 19;9(4):ENEURO.0120-22.2022. [Abstract]
- Chin J Integr Med. 2022 Apr;28(4):319-329. [Abstract]
- PeerJ. 2023 May 25:11:e15407. [Abstract]
- Neurosci Res. 2024 Feb:199:21-29. [Abstract]
- Biomed Res Int. 2021 May 14:2021:5565748. [Abstract]
- Biopharm Drug Dispos. 2022 Dec;43(6):265-271. [Abstract]
- Res Sq. 2024 Sep 19.
- University of Colorado Denver. 2024.
- Research Square Preprint. 2020 Oct.
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WB
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In Vivo Efficacy Study
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Histological Imaging/Staining
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IHC
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ELISA
Biological Activity
KATP[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.0043 μM
Compound: 6 (glyburide)
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Inhibition of human SUR1/Kir6.2 expressed in CHO cells
Inhibition of human SUR1/Kir6.2 expressed in CHO cells
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[PMID: 11356099] |
| CHO | IC50 |
15 μM
Compound: glibenclamide
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Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay
Inhibition of wild type CFTR expressed in CHO cells by [125I]iodide efflux assay
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[PMID: 21397997] |
| HEK293 | IC50 |
1.4 μM
Compound: Glibenclamide
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Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
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[PMID: 22587986] |
| HEK293 | IC50 |
2.2 μM
Compound: Glibenclamide
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Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
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[PMID: 22587986] |
| HEK293 | IC50 |
21 μM
Compound: Glibenclamide
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Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
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[PMID: 22587986] |
| INS-1E | EC50 |
0.003 μM
Compound: glibenclamide
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Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose
Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose
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[PMID: 24484900] |
| INS-1E | EC50 |
0.007 μM
Compound: glibenclamide
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Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose
Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 0.1 mM glucose
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[PMID: 24484900] |
| Mesenchymal stem cells | EC50 |
2.8 μM
Compound: GLI
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Induction of adiponectin secretion in human differentiated BMMSC cells measured at 5 day in the presence of IDX induction medium by ELISA
Induction of adiponectin secretion in human differentiated BMMSC cells measured at 5 day in the presence of IDX induction medium by ELISA
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[PMID: 35172097] |
| Oocyte | IC50 |
0.22 μM
Compound: 6 (glyburide)
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Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes
Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes
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[PMID: 11356099] |
| Sf21 | IC50 |
2.8 μM
Compound: Glibenclamide
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Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| Sf21 | IC50 |
5.3 μM
Compound: Glibenclamide
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Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
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[PMID: 21965623] |
| T-cell line | IC50 |
1 μM
Compound: 2
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In vitro inhibition of Rb efflux in human T-cells; 1-10
In vitro inhibition of Rb efflux in human T-cells; 1-10
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10.1016/S0960-894X(97)00163-7 |
| U-373MG ATCC | IC50 |
>100 μM
Compound: Glibenclamide
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Growth inhibition of human U373 cells after 72 hrs by MTT assay
Growth inhibition of human U373 cells after 72 hrs by MTT assay
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[PMID: 22809560] |
Glibenclamide (Brown adipocytes; 10 μΜ; 1 day) has no effect on adipocyte differentiation. Glibenclamide (Ucp1-2A-GFP brown adipocyte) significantly increases UCP1 expression. Glibenclamide directly binds and blocks the SUR1 subunits of ATP-dependent potassium channels (KATP) and consequently increases insulin secretion from the pancreatic β cells[2]. Glibenclamide interferes with mitochondrial bioenergy by permeating mitochondrial intima with Cl- and promoting mitochondrial net Cl-/K+ cotransport[4]. Glibenclamide induced autophagy inhibits its insulin secretion-improving function in β cells[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Glibenclamide (50 μg/kg; p.o.) does not cause significant change, such as body weight or body composition[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[2]
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Dosage:2 mg/kg
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Administration:P.o.
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Result:Increased of insulin release and rapid drop of blood glucose level.
Chemical Information
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CAS No. 10238-21-8
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Appearance Solid
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Molecular Weight 494.00
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Formula C23H28ClN3O5S
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Color White to off-white
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SMILES
ClC1=CC(C(NCCC2=CC=C(S(NC(NC3CCCCC3)=O)(=O)=O)C=C2)=O)=C(OC)C=C1
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Synonyms
Glyburide
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (28)
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Journal Impact Factor
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Most Recent
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Nat Metab
mPGES-2 blockade antagonizes β-cell senescence to ameliorate diabetes by acting on NR4A1. [Abstract]2022 Feb;4(2):269-283. PMID: 35228744 -
Nat Commun
Cellular senescence-associated gene IFI16 promotes HMOX1-dependent evasion of ferroptosis and radioresistance in glioblastoma. [Abstract]2025 Jan 31;16(1):1212. PMID: 39890789
Glibenclamide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 31;16(1):1212. [Abstract]
Immunoblots of DARTS assay that verified the binding of glyburide (50 µM, 24 h) to IFI16 in U251 cells (n = 3). An unpaired two-tailed t-test was applied. Data are presented as mean ± SD.
Glibenclamide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 31;16(1):1212. [Abstract]
Time response of the mice weight after implantation of U251R cells, on average, the xenograft was locally irradiated with 15 Gy of X-rays, and the mice were administered intragastrically with 1 mg/kg glyburide 2 h before irradiation (N = 5 per group). Data are presented as mean ± SD.
Glibenclamide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 31;16(1):1212. [Abstract]
Representative MRI images of U251R xenografts by T2-weighted MRI at 10-day and 20-day after cell implantation, the whole mount HE-stained brain sections of mice (administered intragastrically with 1 mg/kg glyburide 2 h before irradiation).
Glibenclamide purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 31;16(1):1212. [Abstract]
Glyburide (administered intragastrically with 1 mg/kg glyburide 2 h before irradiation). The positive area of IFI16, HMOX1, and GPX4 in the U251R tumor tissues (N = 5 per group). An unpaired two-tailed t-test was applied. Data are presented as mean ± SD. “n” means the number of individual experiments. “N” represents the number of mice analyzed.
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Pharmacol Res
A novel FFA1 agonist, CPU025, improves glucose-lipid metabolism and alleviates fatty liver in obese-diabetic (ob/ob) mice. [Abstract]2020 Mar;153:104679. PMID: 32014571
Glibenclamide purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2020 Mar;153:104679. [Abstract]
Glucose-dependent insulinotropic effects of CPU025 in MIN6 cells. MIN6 cells were treated with 2 or 25 mM glucose in the absence or presence of Glibenclamide (3 μM).
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Int J Biol Macromol
Duck hepatitis A virus 1-encoded 2B protein disturbs ion and organelle homeostasis to promote NF-κB/NLRP3-mediated inflammatory response. [Abstract]2024 Sep 23:135876. PMID: 39322136 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Br J Pharmacol
HWL-088, a new potent free fatty acid receptor 1 (FFAR1) agonist, improves glucolipid metabolism and acts additively with metformin in ob/ob diabetic mice. [Abstract]2020 May;177(10):2286-2302. PMID: 31971610 -
Cell Rep
Type I unconventional protein secretion of the SARS-CoV-2 nucleocapsid protein promotes inflammatory cytokine release. [Abstract]2026 Jun 25;45(7):117613. PMID: 42360880 -
Int J Nanomedicine
Electromechanical Regulation Underlying Protein Nanoparticle-Induced Osmotic Pressure in Neurotoxic Edema. [Abstract]2025 Apr 5:20:4145-4163. PMID: 40207308 -
Virulence
A. caviae infection triggers IL-1β secretion through activating NLRP3 inflammasome mediated by NF-κB signaling pathway partly in a TLR2 dependent manner. [Abstract]2022 Dec;13(1):1486-1501. PMID: 36040120 -
Pharmaceuticals (Basel)
2025 Sep 21;18(9):1420. PMID: 41011287 -
Front Pharmacol
Hengshun Aromatic Vinegar Improves Glycolipid Metabolism in Type 2 Diabetes Mellitus via Regulating PGC-1α/PGC-1β Pathway. [Abstract]2021 Apr 26:12:641829. PMID: 33981226 -
Eur J Pharmacol
Isoliensinine promotes vasorelaxation and inhibits constriction by regulating the calcium channel in hypertension: In vitro and in vivo approaches. [Abstract]2025 May 23:177765. PMID: 40414594 -
Int Immunopharmacol
Nicorandil restores endothelial cell Kir6.2 expression to alleviate neuropathic pain in mice after chronic constriction injury. [Abstract]2024 Oct 27;143(Pt 2):113494. PMID: 39467345 -
BMC Biol
2021 Mar 3;19(1):40. PMID: 33658023 -
Cancers (Basel)
SAM-Competitive EZH2-Inhibitors Induce Platinum Resistance by EZH2-Independent Induction of ABC-Transporters. [Abstract]2023 Jun 3;15(11):3043. PMID: 37297005 -
Front Cell Dev Biol
Rescue of HSP70 in Spinal Neurons Alleviates Opioids-Induced Hyperalgesia via the Suppression of Endoplasmic Reticulum Stress in Rodents. [Abstract]2020 May 12;8:269. PMID: 32500072
Glibenclamide purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2020 May 12;8:269. [Abstract]
The inhibition of HSP70 releasing by Glibenclamide suppresses morphine-induced ER stress and the phosphorylation of PKA and NR-1. Glibenclamide (200 μM) inhibits the decrease of intracellular HSP70 caused by morphine in SH-SY5Y cells.
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J Cell Physiol
Leptin excites basolateral amygdala principal neurons and reduces food intake by LepRb-JAK2-PI3K-dependent depression of GIRK channels. [Abstract]2024 Feb;239(2):e31117. PMID: 37683049 -
J Periodontal Res
Study on the role of pyroptosis in bone resorption induced by occlusal trauma with or without periodontitis. [Abstract]2022 Jun;57(3):448-460. PMID: 35141913 -
Front Physiol
Roles of Endothelial Motilin Receptor and Its Signal Transduction Pathway in Motilin-Induced Left Gastric Artery Relaxation in Dogs. [Abstract]2021 Oct 28;12:770430. PMID: 34777026 -
eNeuro
PLCβ-Mediated Depletion of PIP2 and ATP-Sensitive K+ Channels Are Involved in Arginine Vasopressin-Induced Facilitation of Neuronal Excitability and LTP in the Dentate Gyrus. [Abstract]2022 Jul 19;9(4):ENEURO.0120-22.2022. PMID: 35788107 -
Chin J Integr Med
Pharmacodynamic Mechanism of Kuanxiong Aerosol for Vasodilation and Improvement of Myocardial Ischemia. [Abstract]2022 Apr;28(4):319-329. PMID: 34897591 -
PeerJ
PFI-3 induces vasorelaxation with potency to reduce extracellular calcium influx in rat mesenteric artery. [Abstract]2023 May 25:11:e15407. PMID: 37250720 -
Neurosci Res
A novel hydrogen sulfide donor reduces neuroinflammation and seizures by activating ATP-sensitive potassium channels. [Abstract]2024 Feb:199:21-29. PMID: 37442198 -
Biomed Res Int
Gentiopicroside Produces Endothelium-Independent Vasodilation by Deactivating the PI3K/Akt/Rho-Kinase Pathway in Isolated Rat Thoracic Aorta. [Abstract]2021 May 14:2021:5565748. PMID: 34095301 -
Biopharm Drug Dispos
Inhibition of canalicular and sinusoidal taurocholate efflux by cholestatic drugs in human hepatoma HepaRG cells. [Abstract]2022 Dec;43(6):265-271. PMID: 36195987 -
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Solvent & Solubility
DMSO : 100 mg/mL (202.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.06 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Heo R, et al. The anti-diabetic drug trelagliptin induces vasodilation via activation of Kv channels and SERCA pumps. Life Sci. 2021;283:119868. [Content Brief]
[2]. Qiu Y, et al. Glyburide Regulates UCP1 Expression in Adipocytes Independent of KATP Channel Blockade. iScience. 2020;23(9):101446. [Content Brief]
[3]. Golstein PE, et al. P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 1999;437(5):652-660. [Content Brief]
[4]. Fernandes MA, et al. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. J Biochem Mol Toxicol. 2004;18(3):162-169. [Content Brief]
[5]. Zhou J, et al. Glibenclamide-Induced Autophagy Inhibits Its Insulin Secretion-Improving Function in β Cells. Int J Endocrinol. 2019;2019:1265175. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0243 mL | 10.1215 mL | 20.2429 mL | 50.6073 mL |
| 5 mM | 0.4049 mL | 2.0243 mL | 4.0486 mL | 10.1215 mL | |
| 10 mM | 0.2024 mL | 1.0121 mL | 2.0243 mL | 5.0607 mL | |
| 15 mM | 0.1350 mL | 0.6748 mL | 1.3495 mL | 3.3738 mL | |
| 20 mM | 0.1012 mL | 0.5061 mL | 1.0121 mL | 2.5304 mL | |
| 25 mM | 0.0810 mL | 0.4049 mL | 0.8097 mL | 2.0243 mL | |
| 30 mM | 0.0675 mL | 0.3374 mL | 0.6748 mL | 1.6869 mL | |
| 40 mM | 0.0506 mL | 0.2530 mL | 0.5061 mL | 1.2652 mL | |
| 50 mM | 0.0405 mL | 0.2024 mL | 0.4049 mL | 1.0121 mL | |
| 60 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.8435 mL | |
| 80 mM | 0.0253 mL | 0.1265 mL | 0.2530 mL | 0.6326 mL | |
| 100 mM | 0.0202 mL | 0.1012 mL | 0.2024 mL | 0.5061 mL |