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.

Physicochemical Properties

Molecular Formula	C17H25NO7
Molecular Weight	355.3829
Exact Mass	355.163
CAS #	80879-63-6
PubChem CID	72004
Appearance	Typically exists as solid at room temperature
Density	1.328g/cm3
Boiling Point	580.2ºC at 760 mmHg
Flash Point	304.7ºC
Index of Refraction	1.584
LogP	0
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	8
Heavy Atom Count	25
Complexity	414
Defined Atom Stereocenter Count	4
SMILES	C(N1C[C@H](O)[C@@H](O)[C@H](O)[C@H]1CO)COC1C=CC(C(=O)OCC)=CC=1
InChi Key	NWWORXYTJRPSMC-CAOSSQGBSA-N
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
Chemical Name	1,5-Dideoxy-1,5-((2-(4-(ethoxycarbonyl)phenoxy)ethyl)imino)-D-glucitol
Synonyms	Emiglitate; Emiglitatum; BAY o 1248; BAY-o-1248; BAY-o 1248; EINECS 279-613-2; Emiglitatum; Emiglitate; UNII-PF8AB2IBUM.
HS Tariff Code	2934.99.9001
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)

Biological Activity

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].
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].
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.

Solubility Data

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

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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (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.