| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
IC50: 956 μM (α-Glucosidase)[1]
alpha-Glucosidase (IC50: 956 uM) |
|---|---|
| ln Vitro |
In vitro enzyme assays demonstrate that Kouitchenside G inhibits alpha-glucosidase with an IC50 value of 956 uM. This inhibitory activity is relatively moderate compared to standard alpha-glucosidase inhibitors such as acarbose. The compound is a naturally occurring xanthone glycoside extracted from Swertia kouitchensis. No other specific biological activities (e.g., antioxidant, anti-inflammatory) have been reported for this compound.
|
| ln Vivo |
No specific in vivo data available for Kouitchenside G. As an alpha-glucosidase inhibitor with moderate potency, it has theoretical potential for postprandial blood glucose reduction in animal models of diabetes. However, the high IC50 value (956 uM) suggests that relatively high concentrations or doses may be required for observable in vivo efficacy. In vivo studies have not been reported in the literature. The compound is primarily used as a natural product reference standard.
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| Enzyme Assay |
Recombinant or yeast alpha-glucosidase enzyme is incubated with varying concentrations of Kouitchenside G (100-5000 uM) in phosphate buffer (pH 6.8) at 37degC for 10 minutes. The substrate p-nitrophenyl-alpha-D-glucopyranoside (pNPG, 5 mM) is added to initiate the reaction. After incubation for 20-30 minutes, the reaction is terminated by adding sodium carbonate (Na2CO3, 1 M). The amount of released p-nitrophenol is measured spectrophotometrically at 405 nm. The percentage of enzyme inhibition is calculated relative to control wells without inhibitor. IC50 values are determined by fitting dose-response curves using non-linear regression analysis (IC50 = 956 uM). Each assay is typically performed in triplicate.
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| Cell Assay |
No published cell-based assays for Kouitchenside G. For intestinal alpha-glucosidase inhibition studies, Caco-2 human intestinal epithelial cells can be used as a model. Cells are cultured in DMEM with 10% FBS and grown to confluence. Differentiated Caco-2 cells express brush border alpha-glucosidases. Cells are treated with Kouitchenside G (100-2000 uM) for 30-60 minutes, followed by addition of maltose or sucrose as substrate. Glucose produced from disaccharide hydrolysis is measured by glucose oxidase-peroxidase (GOD-POD) colorimetric assay. However, the high IC50 value may limit its utility in cell-based systems due to solubility or permeability issues. Cell viability should be assessed by MTT or LDH assay.
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| Animal Protocol |
No published in vivo animal study for Kouitchenside G. Based on its alpha-glucosidase inhibitory activity, a potential in vivo protocol would involve oral administration of Kouitchenside G (50-500 mg/kg) to ICR mice or Sprague-Dawley rats. The compound is formulated in 0.5% carboxymethylcellulose (CMC-Na) or 10% DMSO in saline. After 30 minutes, sucrose or maltose (2 g/kg) is administered orally. Blood samples are collected from the tail vein at 0, 30, 60, and 120 minutes post-glucose load. Blood glucose levels are measured using a glucometer or glucose assay kit. The area under the curve (AUC) for blood glucose is calculated. Reduction in AUC compared to control indicates in vivo alpha-glucosidase inhibition. This protocol has not been validated for this compound.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data for Kouitchenside G. As a high molecular weight glycoside (MW 596.53, LogP -1.4), the compound is hydrophilic and likely has poor oral bioavailability due to low intestinal permeability and susceptibility to hydrolysis by intestinal glycosidases. The sugar moieties may be cleaved by gut microbiota or brush border enzymes prior to absorption. Plasma half-life, Cmax, AUC, clearance, and tissue distribution have not been determined experimentally. The compound is typically stored as a powder at -20degC and is soluble in DMSO.
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| Toxicity/Toxicokinetics |
No specific toxicity data for Kouitchenside G. As a natural product isolated from Swertia kouitchensis, which has been used in traditional medicine, the compound is expected to have low acute toxicity. However, systematic toxicological studies have not been performed. 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.
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| References | |
| Additional Infomation |
Reports indicate that Swertia kouitchensis contains Kouitchenside G, and relevant data is available for reference.
Kouitchenside G (CAS: 1444411-75-9) is a naturally occurring xanthone glycoside isolated from the plant Swertia kouitchensis Franch. (Gentianaceae). It demonstrates inhibitory activity against alpha-glucosidase with an IC50 value of 956 uM. The compound is primarily used as a natural product reference standard and research tool for studying alpha-glucosidase inhibition and anti-diabetic mechanisms. Molecular formula: C27H32O15, molecular weight: 596.53. Appearance: solid at room temperature. Solubility: soluble in DMSO. Storage: powder at -20degC for 3 years; in solvent at -80degC for 6 months. 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 |
C27H32O15
|
|---|---|
| Molecular Weight |
596.534
|
| Exact Mass |
596.174
|
| CAS # |
1444411-75-9
|
| PubChem CID |
71745143
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
-1.4
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
15
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
42
|
| Complexity |
909
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
COC1=CC=CC2=C1OC3=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]([C@H](O5)CO)O)O)O)O)O)O
|
| InChi Key |
MWYPCJMHTQFUAQ-YCPAWSGYSA-N
|
| InChi Code |
InChI=1S/C27H32O15/c1-36-10-6-13-17(18(29)11-4-3-5-12(37-2)25(11)39-13)14(7-10)40-27-24(35)22(33)20(31)16(42-27)9-38-26-23(34)21(32)19(30)15(8-28)41-26/h3-7,15-16,19-24,26-28,30-35H,8-9H2,1-2H3/t15-,16-,19-,20-,21+,22+,23-,24-,26-,27-/m1/s1
|
| Chemical Name |
3,5-dimethoxy-1-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxan-2-yl]oxyxanthen-9-one
|
| 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 | 1.6764 mL | 8.3818 mL | 16.7636 mL | |
| 5 mM | 0.3353 mL | 1.6764 mL | 3.3527 mL | |
| 10 mM | 0.1676 mL | 0.8382 mL | 1.6764 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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