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| 5mg |
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| 25mg |
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Purity: ≥98%
Emiglitate (also known as BAY o 1248) is a novel, potent, selective and competitive inhibitor of α-glucoside hydrolase. Emiglitate is a deoxynojirimycin derivative that acts as an α-glucosidase inhibitor and a powerful inhibitor of glucose-induced insulin release.
| ln Vitro |
In addition to having an inhibitory effect on acid glucan-1,4-alpha-glucosidase and acid alpha-glucosidase activities, emiglitate significantly reduces the release of insulin when glucose is stimulated. On the other hand, when α-glucoside hydrolase inhibitors were present, the activities of acid phosphatase and N-acetyl-β-D-glucosaminidase tended to increase. Emiglitate reversed the effects of CO-induced amplification of glucose-stimulated insulin release and increased acid α-glucoside hydrolase activity, returning it to levels observed in the absence of CO. Emigration had no discernible impact on the CO-induced rise in acid phosphatase or acid N-acetyl-beta-D-glucosaminidase activity [1].
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| ln Vivo |
Emiglitate caused a notable, dose-dependent rise in the concentration of hepatic glycogen in rats that had been fasted. Lysosomal glycogen storage is the only mechanism responsible for the rise in liver glycogen. Emiglitate has a dosage of 5 mg/kg b.wt. does not significantly alter the amounts of EM or the concentration of glycogen [2].
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| 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.
[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 |
| Additional Infomation |
Emiglitate is an organic molecular entity.
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| Molecular Formula |
C17H25NO7
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|---|---|
| Molecular Weight |
355.3829
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| Exact Mass |
355.163
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| CAS # |
80879-63-6
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| PubChem CID |
72004
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.328g/cm3
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| Boiling Point |
580.2ºC at 760 mmHg
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| Flash Point |
304.7ºC
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| Index of Refraction |
1.584
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| LogP |
0
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
25
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| Complexity |
414
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C(N1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO)COC1C=CC(C(=O)OCC)=CC=1
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| InChi Key |
NWWORXYTJRPSMC-CAOSSQGBSA-N
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| InChi Code |
InChI=1S/C17H25NO7/c1-2-24-17(23)11-3-5-12(6-4-11)25-8-7-18-9-14(20)16(22)15(21)13(18)10-19/h3-6,13-16,19-22H,2,7-10H2,1H3/t13-,14-,15+,16+/m0/s1
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| Chemical Name |
1,5-Dideoxy-1,5-((2-(4-(ethoxycarbonyl)phenoxy)ethyl)imino)-D-glucitol
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| Synonyms |
Emiglitate; Emiglitatum; BAY o 1248; BAY-o-1248; BAY-o 1248; EINECS 279-613-2; Emiglitatum; Emiglitate; UNII-PF8AB2IBUM.
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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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