HY-15206-1g | Glibenclamide [10238-21-8] Biotrend USA

Description

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	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]
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]

In Vitro

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.

In Vivo

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.

Clinical Trial

Molecular Weight

494.00

Formula

C₂₃H₂₈ClN₃O₅S

CAS No.

10238-21-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.94%

Select Batch:

SDS (418 KB)

COA (247 KB) HNMR (282 KB) RP-HPLC (242 KB) LCMS (86 KB)

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

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 Related Classifications

Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Autophagy
Potassium Channel Mitochondrial Metabolism Autophagy CFTR P-glycoprotein

Glibenclamide [10238-21-8]

Cat# HY-15206-1g

Brand : MedChemExpress

Other Forms of Glibenclamide:

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Glibenclamide Related Classifications

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Glibenclamide [10238-21-8]

Cat# HY-15206-1g

Brand : MedChemExpress

Other Forms of Glibenclamide:

Glibenclamide Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Glibenclamide Related Classifications

Keywords:

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