| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| Other Sizes |
Purity: ≥98%
Gliquidone (also known as AR-DF 26; Glurenorm; Beglynor) is a potent ATP-sensitive K+ channel antagonist with potential anti0diabetic activity. It inhibits ATP-sensitive K + channel with an IC50 of 27.2 NM. As a sulfonylurea anti-diabetic drug , it is used in the treatment of diabetes mellitus type 2. In patients with type 2 diabetes mellitus, gliquidone reduced the mean plasma glucose levels by 15% and increased insulin levels by 40%. In Caucasian patients with new-onset diabetes mellitus (NODM) after kidney transplantation, gliquidone reduced fasting blood glucose (FBG) from 154 mg/dl to 120 mg/dl.
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| ADME/Pharmacokinetics |
Biological Half-Life
The average terminal half-life is approximately 8 hours (range 5.7–9.4 hours). |
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| References |
Fundam Clin Pharmacol.1991;5(2):107-15;Arzneimittelforschung.1997 Mar;47(3):247-52.
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| Additional Infomation |
1-Cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxo-2-isoquinolinyl)ethyl]phenyl]sulfonylurea belongs to the isoquinoline class of compounds. Gliquidone is a sulfonylurea drug used to treat type 2 diabetes. It is an ATP-dependent potassium channel (KATP channel) blocker. This blocking effect leads to depolarization, which in turn activates voltage-dependent calcium channels, causing calcium ion influx and ultimately increasing insulin release. Gliquidone is a potent second-generation sulfonylurea with hypoglycemic activity. Like other second-generation compounds, gliquidone has a higher affinity for SUR1 and is more potent than first-generation compounds. Furthermore, this drug also has peroxisome proliferation-activated receptor (PPAR) γ-agonist activity. Drug Indications: For the treatment of type 2 diabetes.
Mechanism of Action The mechanism of action of glibenclamide in lowering blood glucose appears to rely on stimulating the release of insulin from functional pancreatic β-cells and increasing the sensitivity of peripheral tissues to insulin. Glibenclamide may bind to ATP-sensitive potassium channel receptors on the surface of pancreatic cells, reducing potassium conductance and leading to cell membrane depolarization. Cell membrane depolarization stimulates the influx of calcium ions through voltage-sensitive calcium channels. The increase in intracellular calcium ion concentration induces insulin secretion. Pharmacodynamics Glibenclamide is a sulfonylurea antidiabetic drug. Diabetic patients lack or have no insulin secreted by the pancreas. Insulin is the primary hormone controlling blood glucose. Glibenclamide is an antidiabetic drug used to treat adult-onset diabetes or non-insulin-dependent diabetes mellitus (NIDDM). Its mechanism of action is to lower blood glucose levels by stimulating the pancreas to produce and release insulin. It also promotes the entry of glucose from the blood into cells that need it. |
| Molecular Formula |
C27H33N3O6S
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|---|---|
| Molecular Weight |
527.63
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| Exact Mass |
527.208
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| CAS # |
33342-05-1
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| Related CAS # |
Gliquidone-d6
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| PubChem CID |
91610
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Melting Point |
179ºC
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| Index of Refraction |
1.624
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| LogP |
3.11
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
37
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| Complexity |
948
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(C1=CC=C(CCN(C(C(C)(C)C2=C3C=C(OC)C=C2)=O)C3=O)C=C1)(NC(NC4CCCCC4)=O)=O
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| InChi Key |
LLJFMFZYVVLQKT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H33N3O6S/c1-27(2)23-14-11-20(36-3)17-22(23)24(31)30(25(27)32)16-15-18-9-12-21(13-10-18)37(34,35)29-26(33)28-19-7-5-4-6-8-19/h9-14,17,19H,4-8,15-16H2,1-3H3,(H2,28,29,33)
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| Chemical Name |
1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxoisoquinolin-2-yl)ethyl]phenyl]sulfonylurea
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| Synonyms |
Gliquidone; Glurenorm; Beglynor; Glikvidon; Glycvidon; Sanofi Synthelabo brand of gliquidone; Yamanouchi brand of gliquidone; AR-DF 26
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.74 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), suspension solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (4.74 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO +Corn oil : 5mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8953 mL | 9.4763 mL | 18.9527 mL | |
| 5 mM | 0.3791 mL | 1.8953 mL | 3.7905 mL | |
| 10 mM | 0.1895 mL | 0.9476 mL | 1.8953 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00568074 | Completed | Drug: repaglinide Drug: Glurenorm® |
Diabetes Diabetes Mellitus, Type 2 |
Novo Nordisk A/S | December 16, 2003 | Phase 4 |
| NCT02475499 | Completed | Drug: DPP-4 inhibitors Drug: GLP-1 analogs |
Diabetes Mellitus, Type 2 | Canadian Network for Observational Drug Effect Studies, CNODES |
March 2014 | |
| NCT02476760 | Completed | Drug: DPP-4 inhibitors Drug: GLP-1 analogs |
Recurrent Glioma Refractory Glioma |
Diabetes Mellitus, Type 2 | March 2014 | |
| NCT02456428 | Completed | Drug: DPP-4 inhibitors Drug: GLP-1 analogs |
Type 2 Diabetes Mellitus | Canadian Network for Observational Drug Effect Studies, CNODES |
March 2014 |
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