| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Glibornuride targets the ATP-sensitive potassium (KATP) channels on pancreatic β-cells. By binding to the sulfonylurea receptor (SUR1) subunit of these channels, it inhibits potassium efflux, leading to membrane depolarization. This opens voltage-gated calcium channels, increasing intracellular calcium and stimulating insulin exocytosis. This mechanism lowers blood glucose levels.
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| ln Vitro |
Glibornuride stimulates insulin release from pancreatic β-cells in vitro. In isolated islet preparations or insulin-secreting cell lines (e.g., MIN6 or INS-1), glibornuride increases insulin secretion in a glucose-dependent manner. The compound's potency and efficacy can be compared to other sulfonylureas such as glibenclamide or glipizide.
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| ln Vivo |
A group of Swiss albino diabetics who received Glibornuride (5 mg/kg; daily gavage for 28 days) had weight increase [2]. For a period of 28 days, glibornuride lowers blood uric acid levels in diabetics [2]. For 28 days, glibornuride was not significant.
Glibornuride lowers blood glucose levels in vivo in diabetic animal models and in humans with type 2 diabetes. Oral administration of glibornuride leads to dose-dependent reductions in fasting and postprandial blood glucose. The compound has been used clinically for the management of type 2 diabetes. Its efficacy is comparable to other sulfonylureas. |
| Enzyme Assay |
The binding of glibornuride to the sulfonylurea receptor (SUR1) on pancreatic β-cell KATP channels can be assessed using radioligand binding assays. Membrane preparations from cells expressing SUR1/Kir6.2 are incubated with [³H]-glibenclamide or [³H]-glyburide in the presence of various concentrations of glibornuride. Competitive displacement of the radioligand is measured, and Ki or IC50 values are calculated.
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| Cell Assay |
Insulin secretion is measured using isolated pancreatic islets or insulin-secreting cell lines. Cells are incubated with glibornuride at various concentrations in glucose-containing buffer, and insulin released into the supernatant is quantified by ELISA or radioimmunoassay. Glucose-stimulated insulin secretion (GSIS) assays are used to assess the compound's ability to enhance glucose-dependent insulin release.
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| Animal Protocol |
Animal/Disease Models: 6-6.5-month-old male Swiss albino rats, body weight 150-200 g[2]
Doses: 5 mg/kg Route of Administration: Daily intragastric (po) (po)administration for 28 days Experimental Results: 28 days Administration resulted in weight gain in the diabetic group. Treatment for 28 days diminished serum uric acid levels in diabetic rats. Glibornuride is administered orally to diabetic animal models (e.g., streptozotocin-induced diabetic rats or db/db mice) or to healthy animals for glucose tolerance tests. Blood glucose levels are measured at various time points post-administration. Oral glucose tolerance tests (OGTT) are performed to assess the compound's ability to improve glucose disposal. Insulin levels can also be measured to confirm the mechanism of action. |
| ADME/Pharmacokinetics |
Glibornuride has a molecular weight of 366.48 and molecular formula C18H26N2O4S. The CAS name is [1S-(endo,endo)]-N-[[(3-Hydroxy-4,7,7-trimethylbicyclo[2.2.1]hept-2-yl)amino]carbonyl]-4-methylbenzenesulfonamide. The compound is well absorbed after oral administration and is metabolized in the liver. It has a half-life suitable for twice-daily dosing. Glibornuride is available as a generic medication.
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| Toxicity/Toxicokinetics |
Sulfonylureas including glibornuride can cause hypoglycemia as a dose-related adverse effect. Other common side effects include weight gain, gastrointestinal disturbances, and rare skin reactions. Hypoglycemia is the most serious adverse effect and can be severe in elderly patients or those with renal impairment. Contraindications include type 1 diabetes, diabetic ketoacidosis, and severe hepatic or renal impairment.
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| References |
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| Additional Infomation |
Glibornuride is a monoterpenoid compound. Glibornuride is a sulfonylurea antidiabetic drug. Glibornuride is a sulfonylurea derivative with high oral bioavailability and hypoglycemic activity. After administration, Glibornuride binds to the sulfonylurea receptor type 1 (SUR1) subunit of the ATP-sensitive inward rectifying potassium channel (K(ATP) channel) on the pancreatic β-cell membrane and blocks its activity. This prevents the influx of positively charged potassium ions (K+) into the cell and induces the influx of calcium ions (Ca2+) through voltage-sensitive calcium channels, thereby triggering the exocytosis of insulin granules. Insulin stimulates glycogen synthesis and inhibits gluconeogenesis; both work together to lower blood glucose levels.
Glibornuride (CAS#: 26944-48-9) is a sulfonylurea anti-diabetic drug used for the treatment of type 2 diabetes. It works by stimulating insulin release from pancreatic β-cells via closure of KATP channels. The compound is a monoterpenoid and is structurally related to other sulfonylureas. Glibornuride is an oral hypoglycemic agent that has been used clinically. It is available as a generic medication and is intended for the management of hyperglycemia in patients with type 2 diabetes. |
| Molecular Formula |
C18H26N2O4S
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|---|---|
| Molecular Weight |
366.479
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| Exact Mass |
366.161
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| CAS # |
26944-48-9
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| PubChem CID |
12818200
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| Appearance |
White to off-white solid powder
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| Density |
1.3g/cm3
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| Melting Point |
192-195° (ethanol-water); also reported as 195-198°
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| Index of Refraction |
1.6
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| LogP |
3.844
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
634
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)NC(=O)N[C@H]2[C@H]3CC[C@@]([C@H]2O)(C3(C)C)C
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| InChi Key |
RMTYNAPTNBJHQI-LLDVTBCESA-N
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| InChi Code |
InChI=1S/C18H26N2O4S/c1-11-5-7-12(8-6-11)25(23,24)20-16(22)19-14-13-9-10-18(4,15(14)21)17(13,2)3/h5-8,13-15,21H,9-10H2,1-4H3,(H2,19,20,22)/t13-,14+,15+,18+/m1/s1
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| Chemical Name |
1-[(1S,2S,3R,4R)-3-hydroxy-4,7,7-trimethyl-2-bicyclo[2.2.1]heptanyl]-3-(4-methylphenyl)sulfonylurea
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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) |
DMSO : ~250 mg/mL (~682.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.68 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 | 2.7287 mL | 13.6433 mL | 27.2866 mL | |
| 5 mM | 0.5457 mL | 2.7287 mL | 5.4573 mL | |
| 10 mM | 0.2729 mL | 1.3643 mL | 2.7287 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.
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