製品番号: HY-15206

グリベンクラミド

(別名: Glibenclamide; Glyburide)

28 Cited Publications

カスタマーレビュー

Based on 28 publication(s) in Google Scholar

Glibenclamide (Glyburide) is an orally active ATP-sensitive K⁺ channel (K_ATP) 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 K_ATP 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.

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純度: 99.83%
CAS 番号: 10238-21-8
分子式: C₂₃H₂₈ClN₃O₅S
分子量:494.00

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Glibenclamide 構造式

CAS 番号: 10238-21-8

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (28)
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- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
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生物活性

製品説明

Glibenclamide (Glyburide) is an orally active ATP-sensitive K⁺ channel (K_ATP) inhibitor and can be used for the research of diabetes and obesity^[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of K_ATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)^[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability^[4]. Glibenclamide can induce autophagy^[5].

IC₅₀ & Target

K_ATP^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.0043 μM Compound: 6 (glyburide)	Inhibition of human SUR1/Kir6.2 expressed in CHO cells Inhibition of human SUR1/Kir6.2 expressed in CHO cells	[PMID: 11356099]
CHO	IC₅₀	15 μM Compound: glibenclamide	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	[PMID: 21397997]
HEK293	IC₅₀	1.4 μM Compound: Glibenclamide	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	[PMID: 22587986]
HEK293	IC₅₀	2.2 μM Compound: Glibenclamide	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate	[PMID: 22587986]
HEK293	IC₅₀	21 μM Compound: Glibenclamide	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	[PMID: 22587986]
INS-1E	EC₅₀	0.003 μM Compound: glibenclamide	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	[PMID: 24484900]
INS-1E	EC₅₀	0.007 μM Compound: glibenclamide	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	[PMID: 24484900]
Mesenchymal stem cells	EC₅₀	2.8 μM Compound: GLI	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	[PMID: 35172097]
Oocyte	IC₅₀	0.22 μM Compound: 6 (glyburide)	Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes Inhibition of human SUR2A/Kir6.2 expressed in Xenopus oocytes	[PMID: 11356099]
Sf21	IC₅₀	2.8 μM Compound: Glibenclamide	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	[PMID: 21965623]
Sf21	IC₅₀	5.3 μM Compound: Glibenclamide	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	[PMID: 21965623]
T-cell line	IC₅₀	1 μM Compound: 2	In vitro inhibition of Rb efflux in human T-cells; 1-10 In vitro inhibition of Rb efflux in human T-cells; 1-10	10.1016/S0960-894X(97)00163-7
U-373MG ATCC	IC₅₀	>100 μM Compound: Glibenclamide	Growth inhibition of human U373 cells after 72 hrs by MTT assay Growth inhibition of human U373 cells after 72 hrs by MTT assay	[PMID: 22809560]

体外実験

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 (K_ATP) 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.

体内実験

Glibenclamide (2 mg/kg; p.o.) increases of insulin release and rapid drop of blood glucose level^[2].
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.

Animal Model:

Mice^[2]
Dosage:

2 mg/kg
Administration:

P.o.
Result:

Increased of insulin release and rapid drop of blood glucose level.

化学情報

CAS 番号 10238-21-8
性状 Solid
分子量 494.00
分子式 C₂₃H₂₈ClN₃O₅S
Color White to off-white
SMILES

ClC1=CC(C(NCCC2=CC=C(S(NC(NC3CCCCC3)=O)(=O)=O)C=C2)=O)=C(OC)C=C1
別名

Glibenclamide; Glyburide
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (28)

All WBELISAIn Vivo Efficacy StudyHistological Imaging/StainingIHC

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Journal Impact Factor

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.
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).
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)

In Vivo Antihypertensive and Ex Vivo Vasodilatory Studies of Taxifolin. [Abstract]

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

GRK2 regulates GLP-1R-mediated early phase insulin secretion in vivo. [Abstract]

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.
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
Res Sq

2024 Sep 19.
University of Colorado Denver

2024.
Research Square Preprint

2020 Oct.

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0243 mL

10.1215 mL

20.2429 mL

5 mM

0.4049 mL

2.0243 mL

4.0486 mL

10 mM

0.2024 mL

1.0121 mL

2.0243 mL

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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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希釈計算機

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濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.06 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg
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g
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Glibenclamide

28 Cited Publications

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MedChemExpress（MCE）の使用を引用している文献 Glibenclamide

生物活性

化学情報

Publications (28)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Glibenclamide 関連分類

HY-15206 関連分類