| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Glibenclamide impurity A is structurally related to glibenclamide, but its primary targets are not the same as the parent drug. It has been identified as an inhibitor of the NLRP3 inflammasome, which plays a role in inflammation. It inhibits the formation of the NLRP3 inflammasome in cardiomyocytes.
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| ln Vitro |
In vitro, Glibenclamide impurity A inhibits the formation of the NLRP3 inflammasome in cardiomyocytes. This activity is distinct from the parent drug's mechanism of action. It is also used as a reference standard in analytical chemistry.
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| ln Vivo |
NLRP3-IN-2 has no influence on the body's glucose levels and is well tolerated [1]. Using NLRP3-IN-2 (100 mg/kg) as a treatment reduced infarction in the ischemia+reperfusion-induced acute myocardial infarction model by 90% (P<0.01) and inhibited the activity of the cardiac inflammasome (caspase-1). Troponin I levels (>70%, P<0.01) and area pathology (>40%, P<0.01) [1].
In vivo, Glibenclamide impurity A limits the infarct size after myocardial ischemia/reperfusion in mice. Treatment with the NLRP3 inhibitor (100 mg/kg) reduced infarction in the ischemia+reperfusion-induced acute myocardial infarction model by 90%. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays are not typically performed for Glibenclamide impurity A, as it is primarily an impurity and reference standard. However, its inhibition of NLRP3 inflammasome formation suggests it may interact with components of the inflammasome complex.
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| Cell Assay |
In vitro cell-based assays for Glibenclamide impurity A involve treating cardiomyocytes to assess its effects on NLRP3 inflammasome formation. Its ability to inhibit inflammasome activation is measured by assessing the activity of caspase-1.
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| Animal Protocol |
Animal/Disease Models: Experimental mouse acute myocardial infarction (AMI) model [1].
Doses: 100 mg/kg. Route of Administration: Administer intraperitoneally (ip) (ip) 30 minutes before surgery, then intraperitoneally (ip) (ip) 3 times every 6 hrs (hrs (hours)). Experimental Results: Caspase-1 activity (reflecting the formation of active inflammasomes) in cardiac tissue measured 24 hrs (hrs (hours)) after ischemia was Dramatically diminished by more than 90%. Resulted in significant reductions in infarct size measured as TTC (>40% reduction) or troponin I levels (>70% reduction) compared with vehicle alone. In vivo animal experiments for Glibenclamide impurity A have been conducted in mouse models of myocardial ischemia/reperfusion injury. The compound is administered at a dose of 100 mg/kg, and its effect on infarct size is assessed. |
| ADME/Pharmacokinetics |
Glibenclamide impurity A has a molecular weight of 368.84 and a molecular formula of C16H17ClN2O4S. It is a pale beige to light yellow solid. Specific pharmacokinetic data is not provided.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Glibenclamide impurity A is not provided in the search results. As an impurity, its safety is assessed in the context of the parent drug's safety profile. Its NLRP3 inhibitory activity suggests a potential therapeutic effect in inflammation.
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| References | |
| Additional Infomation |
Glibenclamide impurity A is an impurity of the antidiabetic drug glibenclamide. It is also known as Glyburide USP Related Compound A. It has been identified as an inhibitor of the NLRP3 inflammasome and has shown efficacy in limiting myocardial infarct size in mice. It is used as a reference standard for quality control.
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| Molecular Formula |
C16H17CLN2O4S
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|---|---|
| Molecular Weight |
368.83
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| Exact Mass |
368.059
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| CAS # |
16673-34-0
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| PubChem CID |
85542
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Melting Point |
209-214 °C
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| Index of Refraction |
1.598
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| LogP |
1.74
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
515
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KVWWTCSJLGHLRM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H17ClN2O4S/c1-23-15-7-4-12(17)10-14(15)16(20)19-9-8-11-2-5-13(6-3-11)24(18,21)22/h2-7,10H,8-9H2,1H3,(H,19,20)(H2,18,21,22)
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| Chemical Name |
5-chloro-2-methoxy-N-[2-(4-sulfamoylphenyl)ethyl]benzamide
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| Synonyms |
Glyburide Related Compound A; Glibenclamide A; Glibenclamide impurity A
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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 : ~125 mg/mL (~338.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.64 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 (5.64 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 | 2.7113 mL | 13.5564 mL | 27.1128 mL | |
| 5 mM | 0.5423 mL | 2.7113 mL | 5.4226 mL | |
| 10 mM | 0.2711 mL | 1.3556 mL | 2.7113 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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