| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
The primary molecular target of Valiolamine is alpha-glucosidase, an enzyme that breaks down carbohydrates into glucose. It acts as a potent competitive inhibitor of α-glucosidases, including sucrase, maltase, and isomaltase. By inhibiting these enzymes, Valiolamine slows the digestion of carbohydrates and reduces postprandial blood glucose levels, making it a potential therapeutic agent for type 2 diabetes.
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|---|---|
| ln Vitro |
In vitro, Valiolamine exhibits potent alpha-glucosidase inhibitory activity against porcine intestinal sucrase, maltase, and isomaltase. It shows significant inhibitory activity against porcine intestinal sucrase and maltase, with Ki values of 30 nM and 350 nM, respectively. This inhibitory activity is more potent than valienamine, validamine, and hydroxyvalidamine, which were reported as building blocks of validamycins and microbial oligosaccharide alpha-glucosidase inhibitors.
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| ln Vivo |
Specific in vivo activity data for Valiolamine are not available in the consulted sources. Its potent alpha-glucosidase inhibitory activity suggests it may have potential for managing postprandial blood glucose levels in vivo. As a competitive inhibitor, it would be expected to be effective when taken with meals. However, no specific in vivo studies have been reported. Further research is needed to evaluate its pharmacokinetics and efficacy in animal models.
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| Enzyme Assay |
Typical in vitro assays for Valiolamine involve measuring alpha-glucosidase activity. Porcine intestinal sucrase, maltase, or isomaltase is incubated with the substrate (sucrose, maltose, or isomaltose) and various concentrations of the compound at 37°C for 15-30 minutes. The glucose produced is measured by the glucose oxidase method, and Ki values are calculated from Lineweaver-Burk plots. These assays allow for detailed characterization of the compound's enzyme inhibition kinetics.
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| Cell Assay |
Cell-based assays for Valiolamine typically involve treating intestinal epithelial cells (e.g., Caco-2 cells) with the compound and measuring alpha-glucosidase activity in cell lysates or on the cell surface. Alternatively, glucose uptake and metabolism can be measured in cells treated with the compound. However, specific assay details for this compound are not available in the consulted sources.
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| Animal Protocol |
In vivo animal experiments for Valiolamine are not detailed in the available literature. For studying alpha-glucosidase inhibitors, typical animal models include carbohydrate-loaded rats or mice, where the compound is administered orally with a carbohydrate load (e.g., sucrose or maltose), and blood glucose levels are measured over time. Such studies have been conducted for other alpha-glucosidase inhibitors like acarbose and voglibose, but not specifically for valiolamine.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Valiolamine are limited. As a small, polar aminocyclitol with a molecular weight of 193.20 g/mol, it would be expected to have poor oral bioavailability due to its hydrophilicity. Alpha-glucosidase inhibitors like acarbose and voglibose are poorly absorbed and act locally in the intestine. Valiolamine is likely similar in this regard. Detailed ADME parameters are not available in the consulted sources.
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| Toxicity/Toxicokinetics |
Toxicological data for Valiolamine are limited. As an aminocyclitol, it is generally considered to have low toxicity. It is a building block of validamycins, which are used as agricultural antibiotics. However, comprehensive toxicological studies have not been reported. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
Valine amine is an aminocyclic alcohol. It has been reported that valine amine has been found in Streptomyces hygroscopicus, and relevant data are available for reference.
Valiolamine is an aminocyclitol with potent alpha-glucosidase inhibitory activity against porcine intestinal sucrase (Ki 30 nM) and maltase (Ki 350 nM). It is more potent than valienamine, validamine, and hydroxyvalidamine. It is a research compound for studying diabetes and carbohydrate metabolism. It is not approved for any clinical indication. |
| Molecular Formula |
C7H15NO5
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|---|---|
| Molecular Weight |
193.20
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| Exact Mass |
118.11
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| CAS # |
83465-22-9
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| PubChem CID |
174312
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| Appearance |
White to off-white solid powder
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| Density |
1.0±0.1 g/cm3
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| Boiling Point |
249.1±25.0 °C at 760 mmHg
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| Flash Point |
104.4±23.2 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.490
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| LogP |
-1.6
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
13
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| Complexity |
190
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1[C@@H]([C@@H]([C@H]([C@@H]([C@]1(CO)O)O)O)O)N
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| InChi Key |
VDLOJRUTNRJDJO-ZYNSJIGGSA-N
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| InChi Code |
InChI=1S/C7H15NO5/c8-3-1-7(13,2-9)6(12)5(11)4(3)10/h3-6,9-13H,1-2,8H2/t3-,4-,5+,6-,7-/m0/s1
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| Chemical Name |
(1S,2S,3R,4S,5S)-5-amino-1-(hydroxymethyl)cyclohexane-1,2,3,4-tetrol
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 5.1760 mL | 25.8799 mL | 51.7598 mL | |
| 5 mM | 1.0352 mL | 5.1760 mL | 10.3520 mL | |
| 10 mM | 0.5176 mL | 2.5880 mL | 5.1760 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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