| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
IC50: 451 μM (α-Glucosidase)[1]
alpha-Glucosidase (IC50: 451 uM) |
|---|---|
| ln Vitro |
In vitro enzyme assays demonstrate that alpha-Glucosidase-IN-24 inhibits yeast alpha-glucosidase with an IC50 of 451 uM. This inhibitory activity is moderate compared to standard alpha-glucosidase inhibitors such as acarbose. The compound is a xanthone glycoside isolated from Swertia kouitchensis. No other specific biological activities (e.g., antioxidant, anti-inflammatory, cytotoxicity) have been reported for this compound. The compound is primarily a natural product reference standard for phytochemical and enzyme inhibition studies.
|
| ln Vivo |
No specific in vivo data available for alpha-Glucosidase-IN-24. As an alpha-glucosidase inhibitor with moderate potency (IC50 451 uM), it has theoretical potential for postprandial blood glucose reduction in animal models of diabetes. However, in vivo efficacy studies have not been reported in the literature. The compound is used primarily as a research reagent for in vitro enzyme inhibition assays and as a natural product standard for analytical chemistry.
|
| Enzyme Assay |
Yeast alpha-glucosidase enzyme (commercially available) is incubated with varying concentrations of alpha-Glucosidase-IN-24 (50-2000 uM) in phosphate buffer (pH 6.8, 100 mM) at 37degC for 10-15 minutes. The substrate p-nitrophenyl-alpha-D-glucopyranoside (pNPG, 5 mM) is added to a final volume of 200 uL to initiate the reaction. After incubation for 20-30 minutes at 37degC, the reaction is terminated by adding sodium carbonate solution (Na2CO3, 1 M, 100 uL). The amount of released p-nitrophenol is measured spectrophotometrically at 405 nm using a microplate reader. The percentage of enzyme inhibition is calculated relative to control wells without inhibitor (containing DMSO vehicle). IC50 values are determined by fitting dose-response curves using non-linear regression analysis with GraphPad Prism or similar software (IC50 = 451 uM). Each assay is typically performed in triplicate. Acarbose (IC50 ~0.1-1 mM) is used as a positive control.
|
| Cell Assay |
No published cell-based assays for alpha-Glucosidase-IN-24. For potential cellular studies, Caco-2 human intestinal epithelial cells can be used. Caco-2 cells are cultured in DMEM supplemented with 10% fetal bovine serum, non-essential amino acids, and antibiotics. Cells are seeded in 96-well plates and grown to confluence for 14-21 days to allow differentiation and expression of brush border alpha-glucosidases. Differentiated cells are treated with alpha-Glucosidase-IN-24 (100-1000 uM) in serum-free medium for 30-60 minutes at 37degC. After treatment, maltose (10 mM) or sucrose (10 mM) is added as substrate and incubated for an additional 30-60 minutes. Glucose produced from disaccharide hydrolysis is measured in the supernatant using a glucose oxidase-peroxidase (GOD-POD) colorimetric assay kit. Cell viability is assessed by MTT or LDH assay to ensure that observed effects are not due to cytotoxicity. However, the high IC50 value may limit its utility in cell-based systems due to solubility or permeability issues.
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| Animal Protocol |
No published in vivo animal study for alpha-Glucosidase-IN-24. Based on its alpha-glucosidase inhibitory activity, a potential in vivo protocol would involve oral administration of alpha-Glucosidase-IN-24 to male ICR mice or Sprague-Dawley rats. The compound is formulated in 0.5% carboxymethylcellulose (CMC-Na) or 10% DMSO in saline due to its moderate hydrophilicity (xanthone glycoside). A typical dosing range would be 50-500 mg/kg, administered by oral gavage 30 minutes before an oral sucrose or maltose load (2 g/kg). Blood samples are collected from the tail vein at 0, 30, 60, and 120 minutes post-sucrose administration. Blood glucose levels are measured using a glucometer or enzymatic glucose assay kit. The area under the curve (AUC) for blood glucose is calculated for 0-120 minutes. Reduction in AUC compared to vehicle-treated control indicates in vivo alpha-glucosidase inhibition. This protocol has not been validated for this specific compound.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data for alpha-Glucosidase-IN-24. As a xanthone glycoside (MW 582.51), the compound is relatively hydrophilic and likely has poor oral bioavailability due to low intestinal permeability. Glycosidic bonds may be hydrolyzed by intestinal brush border enzymes or gut microbiota prior to absorption. The xanthone aglycone may be absorbed if released. Metabolism would occur in the liver via phase I (oxidation, reduction) and phase II (glucuronidation, sulfation) enzymes. Plasma half-life, Cmax, AUC, clearance, and tissue distribution have not been determined. Solubility: soluble in DMSO (typical solubility for natural glycosides). Storage: powder at -20degC for 3 years; in solvent at -80degC for 6 months.
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| Toxicity/Toxicokinetics |
No specific toxicity data for alpha-Glucosidase-IN-24. As a natural product isolated from Swertia kouitchensis (a plant used in traditional medicine), the compound is expected to have low acute toxicity. However, systematic toxicological studies have not been performed. Safety data sheets typically classify the compound as "not a hazardous substance or mixture" under GHS criteria. For research use, standard laboratory safety precautions (gloves, lab coat, eye protection) should be followed. Avoid inhalation, skin contact, and ingestion. Dispose of according to hazardous waste regulations. Not for human use.
|
| References | |
| Additional Infomation |
According to reports, 1-hydroxy-2,6-dimethoxy-8-(6-O-β-D-xylanopyranosyl-β-D-glucopyranosyloxy)xanthone has been discovered in Swertia kouitchensis, and relevant data are available.
alpha-Glucosidase-IN-24 (Compound 13, CAS: 60354-05-4) is a naturally occurring alpha-glucosidase inhibitor isolated from the plant Swertia kouitchensis Franch. (Gentianaceae). The compound belongs to the xanthone glycoside class of natural products. It demonstrates inhibitory activity against yeast alpha-glucosidase with an IC50 of 451 uM. alpha-Glucosidase-IN-24 is primarily used as a research reagent for in vitro enzyme inhibition studies and as a natural product standard for phytochemical analysis. It is also known as a xanthone glycoside constituent of Swertia kouitchensis. Molecular formula: C26H30O15, molecular weight: 582.51. Appearance: solid. Solubility: soluble in DMSO. Storage: store as powder at -20degC. Shipping: room temperature stable. Not approved for clinical use. Reference: Wan LS, et al. Xanthone glycoside constituents of Swertia kouitchensis with alpha-glucosidase inhibitory activity. J Nat Prod. 2013;76(7):1248-53. |
| Molecular Formula |
C26H30O15
|
|---|---|
| Molecular Weight |
582.507
|
| Exact Mass |
582.158
|
| CAS # |
60354-05-4
|
| PubChem CID |
72163130
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
-1.1
|
| Hydrogen Bond Donor Count |
7
|
| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
41
|
| Complexity |
893
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
COC1=C(C2=C(C=C1)OC3=C(C2=O)C(=CC(=C3)OC)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO[C@H]5[C@@H]([C@H]([C@@H](CO5)O)O)O)O)O)O)O
|
| InChi Key |
NNYKTKDAAWADQG-HBSGFRINSA-N
|
| InChi Code |
InChI=1S/C26H30O15/c1-35-9-5-13-16(21(31)17-11(39-13)3-4-12(36-2)19(17)29)14(6-9)40-26-24(34)22(32)20(30)15(41-26)8-38-25-23(33)18(28)10(27)7-37-25/h3-6,10,15,18,20,22-30,32-34H,7-8H2,1-2H3/t10-,15-,18+,20-,22+,23-,24-,25+,26-/m1/s1
|
| Chemical Name |
1-hydroxy-2,6-dimethoxy-8-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2S,3R,4S,5R)-3,4,5-trihydroxyoxan-2-yl]oxymethyl]oxan-2-yl]oxyxanthen-9-one
|
| 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)
|
| 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 | 1.7167 mL | 8.5835 mL | 17.1671 mL | |
| 5 mM | 0.3433 mL | 1.7167 mL | 3.4334 mL | |
| 10 mM | 0.1717 mL | 0.8584 mL | 1.7167 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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