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Published TCIMAIL newest issue No.199
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CAS RN: 21187-98-4 | Product Number: G0381
Gliclazide
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Purity: >98.5%(T)(HPLC)
Synonyms:
- 1-[3-Azabicyclo[3.3.0]oct-3-yl]-3-p-toluenesulfonylurea
Product Documents:
| Size | Unit Price | Belgium | Japan* | Quantity |
|---|---|---|---|---|
| 5G |
€64.00
|
1 | 2 |
|
*Stock available in Belgium will be delivered in 1 to 3 days
*Stock available in Japan will be delivered in 1 to 2 weeks (excludes regulated items and dry ice shipments).
| Product Number | G0381 |
Purity / Analysis Method 
|
>98.5%(T)(HPLC) |
| Molecular Formula / Molecular Weight | C__1__5H__2__1N__3O__3S = 323.41 |
| Physical State (20 deg.C) | Solid |
| Storage Temperature
|
Room Temperature (Recommended in a cool and dark place, <15°C) |
| CAS RN | 21187-98-4 |
| Reaxys Registry Number | 1657836 |
| PubChem Substance ID | 135726993 |
| Merck Index (14) | 4439 |
| MDL Number | MFCD00409893 |
Specifications
| Appearance | White to Almost white powder to crystal |
| Purity(HPLC) | min. 98.5 area% |
| Purity(Neutralization titration) | min. 98.5 % |
| Melting point | 165.0 to 169.0 °C |
| NMR | confirm to structure |
Properties (reference)
| Melting Point | 167 °C |
| Solubility in water | Insoluble |
| Solubility (soluble in) | Dimethylformamide |
| Solubility (slightly sol. in) | Ethanol, Methanol |
GHS
Related Laws:
| EC Number | 244-260-5 |
| RTECS# | YT4500000 |
Transport Information:
| HS Number | 2933998090 |
Application
Gliclazide: A Sulfonylurea ATP-Dependent K+ Channel Antagonist
Gliclazide belongs to sulfonylurea antidiabetics which increase the release of insulin from pancreatic B-cells. Sulfonylurea antidiabetics inhibit ATP-gated K+ channels and thereby cause depolarization of the B-cell membrane. The depolarization leads to activation of voltage-dependent Ca channels and Ca2+ influx into the B-cell, and eventually increases insulin release. Gliclazide also has hemovascular properties, such as the anti-oxidant, platelet inhibiting and fibrinolytic actions. In addition, gliclazide is characterized by poor solubility in water. Therefore, it has been studied to improve the solubility and bioavailability of drug. (The product is for research purpose only.)
References
- Gliclazide. An update of its pharmacological properties and therapeutic efficacy in non-insulin-dependent diabetes mellitus (a review)
- Sulfonylurea stimulation of insulin secretion (a review)
- Gliclazide modified release (a review)
- Improvement of water solubility and in vitro dissolution rate of gliclazide by complexation with β-cyclodextrin
- Enhancement of dissolution rate of gliclazide using solid dispersions with polyethylene glycol 6000
- Cogrinding as an approach to enhance dissolution rate of a poorly water-soluble drug (gliclazide)
- The development and validation of liquid chromatography method for the simultaneous determination of metformin and glipizide, gliclazide, glibenclamide, or glimperide in plasma
Application
Study of Sulfonylureas Receptors
References
- The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated potassium channel in insulin-secreting cells
- H. Schmid-Antomarchi, L. De Weille, M. Fosset, M. Lazdunski, J. Biol. Chem. 1987, 262, 15840.
- Antidiabetic sulfonylureas control action potential properties in heart cells via high affinity receptors that are linked to ATP-dependent potassium channels
- M. Fosset, J. R. De Weille, R. D. Green, H. Schmid-Antomarchi, M. Lazdunski, J. Biol. Chem. 1988, 263, 7933.
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