Emiglitate (BAY o 1248) |
| カタログ番号GC31425 |
エミグリテート (BAY o 1248) (BAY o 1248) は、α-グルコシド加水分解酵素の強力な選択的競合阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 80879-63-6
Sample solution is provided at 25 µL, 10mM.
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Emiglitate (BAY o 1248) is a potent, selective and competitive inhibitor of α-glucoside hydrolase.
Emiglitate greatly suppresses the glucose-stimulated insulin release in parallel with an inhibitory effect on the activities of acid glucan-1,4-α-glucosidase and acid α-glucosidase. In contrast, the activities of acid phosphatase and N-acetyl-β-D-glucosaminidase tend to increase in the presence of the α-glucoside hydrolase inhibitor. The CO-induced amplification of the glucose-stimulated insulin release as well as of the increased activities of the acid α-glucoside hydrolases are abrogated by emiglitate and displayed the same levels as in the absence of CO. The CO-induced rise in the activities of acid phosphatase and acid N-acetyl-β-D-glucosaminidase is not appreciably affected by emiglitate[1].
In fasted rats, emiglitate inducec a significant, dose-dependent increase of hepatic glycogen concentrations. The increase in hepatic glycogen is due to lysosomal storage of glycogen only. Emiglitate in the amount of 5 mg/kg b.wt. does not induce significant changes either of glycogen concentrations or at the EM-level[2].
[1]. Mosén H, et al. Nitric oxide inhibits, and carbon monoxide activates, islet acid alpha-glucoside hydrolase activitiesin parallel with glucose-stimulated insulin secretion. J Endocrinol. 2006 Sep;190(3):681-93. [2]. Lembcke B, et al. Lysosomal storage of glycogen as a sequel of alpha-glucosidase inhibition by the absorbed deoxynojirimycin derivative emiglitate (BAYo1248). A drug-induced pattern of hepatic glycogen storage mimicking Pompe's disease (glycogenosis type II). Res Exp Med (Berl). 1991;191(6):389-404.
Kinase experiment: | Effect of the selective α-glucoside hydrolase inhibitor emiglitate (100 μM) on glucose-stimulated insulin secretion and islet lysosomal enzyme activities at 12 mM glucose in the absence and presence of CO gas is studied. Islets are incubated in the absence (open columns) or presence (solid columns) of emiglitate. Experiments are performed both in the presence (the two columns to the right) and in the absence (the two columns to the left) of exogenous CO[1]. |
References: [1]. Mosén H, et al. Nitric oxide inhibits, and carbon monoxide activates, islet acid alpha-glucoside hydrolase activitiesin parallel with glucose-stimulated insulin secretion. J Endocrinol. 2006 Sep;190(3):681-93. | |
| Cas No. | 80879-63-6 | SDF | |
| Canonical SMILES | O=C(OCC)C1=CC=C(OCCN2[C@H](CO)[C@@H](O)[C@H](O)[C@@H](O)C2)C=C1 | ||
| Formula | C17H25NO7 | M.Wt | 355.38 |
| 溶解度 | Soluble in DMSO | 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 | 2.8139 mL | 14.0694 mL | 28.1389 mL |
| 5 mM | 0.5628 mL | 2.8139 mL | 5.6278 mL |
| 10 mM | 0.2814 mL | 1.4069 mL | 2.8139 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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