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| Targets |
Glyparamide targets the sulfonylurea receptor (SUR) on pancreatic beta-cells. As a sulfonylurea, it binds to the SUR subunit of the ATP-sensitive potassium (KATP) channel, closing the channel and depolarizing the cell membrane. This depolarization opens voltage-gated calcium channels, increasing intracellular calcium and stimulating insulin secretion. The compound's hypoglycemic activity is mediated through this mechanism.
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| ln Vitro |
In vitro, glyparamide shows hypoglycemic activity. As a sulfonylurea, its activity has been characterized in insulin secretion assays using pancreatic beta-cell lines or isolated pancreatic islets. The compound stimulates insulin release in a glucose-dependent manner. Its effects on platelet aggregation have also been demonstrated in vitro.
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| ln Vivo |
In vivo, glyparamide is an orally active hypoglycemic agent used to control blood sugar levels in type 2 diabetes. It shows hypoglycemic activity and rarely causes hepatic injury. The compound also reduces platelet aggregation and atherosclerotic plaque formation. Its oral bioavailability makes it suitable for clinical use as an antidiabetic agent.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for glyparamide involves measuring its binding to the sulfonylurea receptor (SUR). Membrane preparations from pancreatic beta-cells or cells expressing SUR are incubated with radiolabeled sulfonylurea (e.g., 3H-glibenclamide) and varying concentrations of glyparamide (typically 0.001-100 uM) in binding buffer at room temperature for 1-2 hours. Bound and free ligand are separated by filtration, and radioactivity is measured by scintillation counting. The inhibition constant (Ki) is calculated from IC50 values. For insulin secretion studies, pancreatic beta-cell lines or isolated islets are treated with glyparamide and insulin release is measured by ELISA or RIA.
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| Cell Assay |
In vitro cellular assays for glyparamide are conducted using pancreatic beta-cell lines such as INS-1 or MIN6 cells. Cells are seeded in multi-well plates and treated with varying concentrations of glyparamide (typically 0.01-100 uM) in the presence of varying glucose concentrations (typically 2-20 mM) for 1-4 hours. Insulin secretion into the culture medium is measured by ELISA or RIA. Cell viability is monitored using MTT or similar assays. For platelet aggregation studies, platelet-rich plasma is treated with glyparamide and aggregation is induced by ADP or collagen, and aggregation is measured by turbidimetry.
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| Animal Protocol |
In vivo animal studies for glyparamide typically involve administration to rodent models of type 2 diabetes such as db/db mice or Zucker diabetic fatty rats. The compound is administered by oral gavage at doses ranging from 1-50 mg/kg/day for 2-8 weeks. Blood glucose levels are measured at regular intervals using a glucometer. Glucose tolerance tests (OGTT) are performed to assess glucose handling. Insulin levels are measured by ELISA. Platelet aggregation and atherosclerotic plaque formation can be assessed in appropriate models. At study termination, tissues are harvested for histological examination.
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| ADME/Pharmacokinetics |
Glyparamide is an orally active sulfonylurea with a molecular weight of 353.82 and a molecular formula of C15H16ClN3O3S. It is a chlorophenyl-containing sulfonylurea that is well absorbed after oral administration. The compound is metabolized in the liver and excreted via urine and feces. Its pharmacokinetic profile is consistent with other sulfonylurea antidiabetic agents. The compound should be stored at -80degC.
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| Toxicity/Toxicokinetics |
The toxicological profile of glyparamide is characteristic of sulfonylureas. The compound rarely causes liver damage. Common side effects include hypoglycemia, weight gain, and gastrointestinal disturbances. The compound is for research use only and is not intended for human therapeutic use. Standard safety precautions should be followed when handling the compound in a laboratory setting. No specific LD50 values have been reported.
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| References | |
| Additional Infomation |
Glipizide is a sulfonylurea hypoglycemic drug containing chlorophenyl groups. Glipizide rarely causes liver damage.
Glyparamide (CAS 5581-42-0) is an orally bioactive chlorophenyl-containing sulfonylurea with hypoglycemic activity. It is used to control blood sugar levels in type 2 diabetes and reduces platelet aggregation and atherosclerotic plaque formation. The compound rarely causes liver damage and is available for research purposes only. |
| Molecular Formula |
C15H16N3O3SCL
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|---|---|
| Molecular Weight |
353.82384
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| Exact Mass |
353.06
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| CAS # |
5581-42-0
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| PubChem CID |
246940
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| Appearance |
White to off-white solid powder
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| Density |
1.41g/cm3
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| Index of Refraction |
1.638
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| LogP |
4.461
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
491
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
SUQZXLUIKZXADU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H16ClN3O3S/c1-19(2)13-7-5-12(6-8-13)17-15(20)18-23(21,22)14-9-3-11(16)4-10-14/h3-10H,1-2H3,(H2,17,18,20)
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| Chemical Name |
1-(4-chlorophenyl)sulfonyl-3-[4-(dimethylamino)phenyl]urea
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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 : ~55 mg/mL (~155.45 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (7.77 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 27.5 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: ≥ 2.75 mg/mL (7.77 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 27.5 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: ≥ 2.75 mg/mL (7.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8263 mL | 14.1315 mL | 28.2630 mL | |
| 5 mM | 0.5653 mL | 2.8263 mL | 5.6526 mL | |
| 10 mM | 0.2826 mL | 1.4131 mL | 2.8263 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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