Diazoxide-d3 |
| カタログ番号GC46131 |
ジアゾキシドの定量化のための内部標準
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1432063-51-8
Sample solution is provided at 25 µL, 10mM.
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Diazoxide-d3 is intended for use as an internal standard for the quantification of diazoxide by GC- or LC-MS. Diazoxide is an activator of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = 14.1 μM in a FLIPR assay using HEK293 cells).1 It also activates SUR2A/Kir6.2 and SUR2B/Kir6.2 channels in HEK293T cells in a patch-clamp assay when used at concentrations of 30 and 300 μM.2 Diazoxide inhibits glucose-induced insulin release from isolated rat pancreatic β cells and induces relaxation of isolated rat aortic rings precontracted with potassium chloride (IC50s = 22.6 and 22.4 μM, respectively).3 It reduces mean arterial pressure and cerebral blood flow in spontaneously hypertensive rats when administered intravenously as a 5 mg/kg bolus dose.4 Diazoxide (50 mg/kg, i.p.) increases blood glucose levels in mice.5 Formulations containing diazoxide have been used in the treatment of hypoglycemia.
|1. Gopalakrishnan, M., Molinari, E.J., Char-Change, S., et al. Pharmacology of human sulphonylurea receptor SUR1 and inward rectifier K+ channel Kir6.2 combination expressed in HEK-293 cells. Br. J. Pharmacol. 129(7), 1323-1332 (2000).|2. Matsuoka, T., Matsushita, K., Katayama, Y., et al. C-Terminal tails of sulfonylurea receptors control ADP-induced activation and diazoxide modulation of ATP-sensitive K+ channels. Circ. Res. 87(10), 873-880 (2000).|3. de Tullio, P., Becker, B., Boverie, S., et al. Toward tissue-selective pancreatic B-cells KATP channel openers belonging to 3-alkylamino-7-halo-4H-1,2,4-benzothiadiazine 1,1-dioxides. J. Med. Chem. 46(15), 3342-3353 (2003).|4. Barry, D.I., Strandgaard, S., Graham, D.I., et al. Effect of diazoxide-induced hypotension on cerebral blood flow in hypertensive rats. Eur. J. Clin. Invest. 13(3), 201-207 (1983).|5. Foy, J.M., and Furman, B.L. Effect of single dose administration of diuretics on the blood sugar of alloxan-diabetic mice or mice made hyperglycaemic by the acute administration of diazoxide. Br. J. Pharmacol. 47(1), 124-132 (1973).
| Cas No. | 1432063-51-8 | SDF | |
| Canonical SMILES | ClC1=CC=C(NC(C([2H])([2H])[2H])=NS2(=O)=O)C2=C1 | ||
| Formula | C8H4ClD3N2O2S | M.Wt | 233.7 |
| 溶解度 | DMSO: slightly soluble | 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. |
||
| 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 | 4.279 mL | 21.395 mL | 42.7899 mL |
| 5 mM | 0.8558 mL | 4.279 mL | 8.558 mL |
| 10 mM | 0.4279 mL | 2.1395 mL | 4.279 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 40 reference(s) in Google Scholar.)
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