Size | Price | Stock | Qty |
---|---|---|---|
1g |
|
||
2g |
|
||
5g |
|
||
10g |
|
||
Other Sizes |
|
Purity: ≥98%
Glyburide (formerly HB419; HB420; Glibenclamide; Micronase; Diabeta; Maninil; Micronase; Neogluconin) is a selective blocker of vascular ATP-sensitive K+ channels (KATP) that has been approved as an antidiabetic sulfonylurea drug used for the treatment of type 2 diabetes. Its actions are similar to those of chlorpropamide that can potentially be used to decrease cerebral edema.
ln Vitro |
Glibenclamide (brown adipocytes; 10 μM; 1 day) has no effect on adipocyte differentiation. Glibenclamide (Ucp1-2A-GFP brown adipocyte) dramatically increases UCP1 expression. Glibenclamide directly binds to and inhibits the SUR1 subunit of ATP-dependent potassium channels (KATP), consequently boosting insulin production from pancreatic beta cells [2]. Glibenclamide interferes with mitochondrial bioenergetics by allowing Cl- to enter the inner mitochondrial membrane and boosting Cl-/K+ co-transport in the mitochondrial network [4]. Glibenclamide-induced autophagy limits its beneficial effect on β-cell insulin secretion [5].
|
---|---|
ln Vivo |
Glibenclamide (2 mg/kg; po) quickly lowers blood glucose levels and enhances the release of insulin [2]. Body weight and body composition do not significantly alter when using glibeenclamide (50 μg/kg; po) [2].
|
Animal Protocol |
Animal/Disease Models: Mice[2]
Doses: 2 mg/kg Route of Administration: Po Experimental Results: Increased of insulin release and rapid drop of blood glucose level. |
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.
[2]. Qiu Y, et al. Glyburide Regulates UCP1 Expression in Adipocytes Independent of KATP Channel Blockade. iScience. 2020;23(9):101446. [3]. Golstein PE, et al. P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 1999;437(5):652-660. [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. [5]. Zhou J, et al. Glibenclamide-Induced Autophagy Inhibits Its Insulin Secretion-Improving Function in β Cells. Int J Endocrinol. 2019;2019:1265175. |
Molecular Formula |
C23H28CLN3O5S
|
|
---|---|---|
Molecular Weight |
494
|
|
CAS # |
10238-21-8
|
|
Related CAS # |
Glyburide-d3;1219803-02-7;Glyburide-d11;1189985-02-1
|
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
|
SMILES |
ClC1C([H])=C([H])C(=C(C=1[H])C(N([H])C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])S(N([H])C(N([H])C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])=O)(=O)=O)=O)OC([H])([H])[H]
|
|
InChi Key |
ZNNLBTZKUZBEKO-UHFFFAOYSA-N
|
|
InChi Code |
InChI=1S/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29)
|
|
Chemical Name |
5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide
|
|
Synonyms |
|
|
HS Tariff Code |
2934.99.9001
|
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.