| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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Glibornuride (trade name Glutril) is an approved orally bioavailable anti-diabetic drug in Switzerland that belongs to the group of sulfonylureas. It acts as a novel and potent blocker of adenosine 5'-triphosphate (ATP)-sensitive K+ channels (KATP channels) with antihyperglycemic activity. Glibornuride is an . It has been shown to antagonize the relaxant response to the K+ channel opener cromakalim and produce airway smooth muscle relaxation. It is associated with lactic acidosis and hypoglycemia in patients with type 2 diabetes melitus.
| 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.
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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. |
| References |
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| Additional Infomation |
Glibornuride is a monoterpenoid.
Glibornuride is a sulfonylurea-type anti-diabetic drug. Glibornuride is an orally bioavailable sulfonamide urea derivative with antihyperglycemic activity. Upon administration, glibornuride binds to and blocks the sulfonylurea receptor type 1 (SUR1) subunit of the ATP-sensitive inwardly-rectifying potassium (K(ATP)) channels on the membranes of pancreatic beta cells. This prevents the inward flow of positively charged potassium (K+) ions into the cell, and induces a calcium ion (Ca2+) influx through voltage-sensitive calcium channels, which triggers exocytosis of insulin-containing granules. Insulin stimulates glycogen synthesis and inhibits gluconeogenesis, which together lower blood glucose levels. |
| Molecular Formula |
C18H26N2O4S
|
|---|---|
| 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
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
25
|
| Complexity |
634
|
| Defined Atom Stereocenter Count |
4
|
| 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
|
| InChi Key |
RMTYNAPTNBJHQI-LLDVTBCESA-N
|
| 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
|
| 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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