Name: Glyburide (Glibenclamide)
Brand: Selleck Chemicals
SKU: S1716
Availability: InStock
Rating: 5 (10 reviews)

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Quality Control

Batch: Purity: 99.93%

99.93

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel GABA Receptor TRP Channel ATPase GluR
Other Potassium Channel Inhibitors	Nigericin TRAM-34 Nicorandil ML133 HCl Hydralazine HCl Sophocarpine Senicapoc (ICA-17043) Gliquidone Butamben PAP-1

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
INS-1E cells	Function assay	1 h	Stimulation of insulin secretion in rat INS-1E cells after 1 hr by alphaLISA assay in presence of 5 mM glucose, EC50=0.003 μM
CHO cells	Function assay		Inhibition of human SUR1/Kir6.2 expressed in CHO cells, IC50=0.0043 μM
HEK293 cells	Function assay		Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate, IC50=1.4 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 99 mg/mL (200.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (20.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	494	Formula	C₂₃H₂₈ClN₃O₅S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	10238-21-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Glibenclamide			SMILES	COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	Potassium channel
In vitro	Glyburide (Glibenclamide), 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. This compound increases the apparent affinity of HDL binding to Scavenger receptor class B type I (SR-BI). It 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). At 6 mM, it reduces the opening of KATP channels, aggravating Ca2+ loading only when applied to dinitrophenol-pretreated myocytes but not when applied with dinitrophenol treatment. In concentrations of 10-500 nM, it produces a dose-dependent inhibition of the potassium channel openers (PCOs) relaxation time course. It also reverses existing Pinacidil relaxation regardless of the degree of pre-existing relaxation, and is able to produce its blockade regardless of the state of K+ channel activation.
In vivo	S1716 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. S1716 (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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/2464055/ [2] https://pubmed.ncbi.nlm.nih.gov/15102890/ [3] https://pubmed.ncbi.nlm.nih.gov/8858310/ [4] https://pubmed.ncbi.nlm.nih.gov/8435468/ [5] https://pubmed.ncbi.nlm.nih.gov/8496833/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-10-28)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07221799	NOT_YET_RECRUITING	Multiple Sclerosis; Neuropathic Pain	University of Maryland, Baltimore	2026-09-01	PHASE1
NCT05426681	RECRUITING	Acute Spinal Cord Injury	Francis Farhadi	2022-07-07	PHASE1
NCT07802561	RECRUITING	Gestational Diabetes Mellitus (GDM)	Nishtar Medical University	2026-04-18	PHASE4
NCT06589141	UNKNOWN	Gestational Diabetes Mellitus in Pregnancy	Assiut University	2025-01-01
NCT05687500	ACTIVE_NOT_RECRUITING	Transient; Hypoglycemia, Neonatal; Preterm; Glibenclamide Adverse Reaction	Assistance Publique - Hôpitaux de Paris	2023-05-20	PHASE2
NCT05688332	UNKNOWN	Diabetes Mellitus Type 2 Without Complication	University of Zambia	2023-08	PHASE3

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Glyburide (Glibenclamide) Potassium Channel inhibitor

Chemical Structure

Molecular Weight: 494