Glyburide-d3 (Synonyms: Glibenclamide-d3) |
| Catalog No.GC47406 |
An internal standard for the quantification of glyburide
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1219803-02-7
Sample solution is provided at 25 µL, 10mM.
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Glyburide-d3 is intended for use as an internal standard for the quantification of glyburide by GC- or LC-MS. Glyburide is a sulfonylurea and an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (IC50 = 4.3 nM).1 It binds to microsomes derived from RINm5F pancreatic β-cells (Kd = 0.3 nM) and inhibits 86Rb+ efflux from intact RINm5 cells with a half-maximal inhibition (K0.5) value of 0.06 nM.2 Glyburide (5 mg/kg) reduces blood glucose levels and increases the activity of hepatic glutathione-S-transferase (GST) and glucose-6-phosphate dehydrogenase (G6PDH) in a rat model of diabetes induced by streptozotocin .3 It inhibits ATP-induced increases in caspase-1 activation and IL-1β and IL-18 secretion in a concentration-dependent manner in LPS-primed bone marrow-derived macrophages (BMDMs).4 Glyburide (80 mg/ml) also reduces lesion growth in mice infected with L. mexicana.5 Formulations containing glyburide have been used in the treatment of type 2 diabetes.
1.Coghlan, M.J., Carroll, W.A., and Gopalakrishnan, M.Recent developments in the biology and medicinal chemistry of potassium channel modulators: Update from a decade of progressJ. Med. Chem.44(11)1627-1653(2001) 2.Schmid-Antomarchi, H., De Weille, J., Fosset, M., et al.The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated K+ channel in insulin-secreting cellsThe Journal of Biological Chemisty262(33)15840-15844(1987) 3.Bugdayci, G., Altan, N., Sancak, B., et al.The effect of the sulfonylurea glyburide on glutathione-S-transferase and glucose-6-phosphate dehydrogenase in streptozotocin-induced diabetic rat liverActa. Diabetol.43(4)131-134(2006) 4.Lamkanfi, M., Mueller, J.L., Vitari, A.C., et al.Glyburide inhibits the Cryopyrin/Nalp3 inflammasomeJournal of Cell Biology187(1)61-70(2009) 5.Serrano-MartÍn, X., Payares, G., and Mendoza-LeÓn, A.Glibenclamide, a blocker of K+ATP channels, shows antileishmanial activity in experimental murine cutaneous leishmaniasisAntimicrobial Agents and Chemotherapy50(12)4214-4216(2006)
| Cas No. | 1219803-02-7 | SDF | |
| Synonyms | Glibenclamide-d3 | ||
| Canonical SMILES | ClC1=CC(C(NCCC2=CC=C(S(NC(NC3CCCCC3)=O)(=O)=O)C=C2)=O)=C(OC([2H])([2H])[2H])C=C1 | ||
| Formula | C23H25ClD3N3O5S | M.Wt | 497 |
| Solubility | DMSO : 250 mg/mL (503.00 mM; Need ultrasonic); H2O : 0.1 mg/mL (0.20 mM; Need ultrasonic and warming) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0121 mL | 10.0604 mL | 20.1207 mL |
| 5 mM | 0.4024 mL | 2.0121 mL | 4.0241 mL |
| 10 mM | 0.2012 mL | 1.006 mL | 2.0121 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
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