| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
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| Targets |
Swertisin targets multiple proteins. It is an oral adenosine A1 receptor antagonist, which may contribute to its cognitive-enhancing effects. It is also an inhibitor of sodium-glucose cotransporter 2 (SGLT2), a target for anti-diabetic drugs, which explains its antihyperglycemic action. Its antioxidant properties are mediated through its ability to scavenge free radicals. Its inhibition of HBV suggests it may target viral replication enzymes.
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| ln Vitro |
In vitro, Swertisin has been shown to have anti-diabetic, antioxidant, and anti-HBV activities. It inhibits SGLT2 in HEK293 cells. It efficiently changes the morphology of NIH3T3 cells from fibroblastic to round aggregate cell clusters, indicating its potential to induce differentiation. Its antioxidant properties are measured using standard cell-free and cell-based assays.
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| ln Vivo |
In vivo, Swertisin improves cognitive and memory impairments in mice. Its anti-diabetic activity has been demonstrated in animal models, where it shows a strong antihyperglycemic action. These effects are attributed to its SGLT2 inhibition and adenosine A1 receptor antagonism. It is a promising candidate for the treatment of diabetes and cognitive disorders.
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| Enzyme Assay |
In vitro non-cell enzyme assays for Swertisin involve measuring its inhibition of SGLT2 and its binding to the adenosine A1 receptor. For SGLT2 inhibition, the compound is incubated with the transporter and a labeled substrate, and the inhibition of substrate uptake is measured. Receptor binding assays use membrane preparations and radiolabeled ligands.
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| Cell Assay |
In vitro cell-based assays for Swertisin use HEK293 cells expressing SGLT2 to study its inhibitory activity. Its effects on glucose uptake are measured. The compound's ability to induce differentiation is studied in NIH3T3 cells. Its antioxidant effects are assessed in cells exposed to oxidative stress. Its anti-HBV activity is measured in HBV-infected cell lines.
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| Animal Protocol |
In vivo animal studies for Swertisin employ models of diabetes and cognitive impairment. For diabetes, mice are treated with the compound, and blood glucose levels and glucose tolerance are measured. For cognitive studies, mouse models of memory impairment are used, and cognitive function is assessed using behavioral tests.
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| ADME/Pharmacokinetics |
Swertisin has a molecular weight of 446.41 g/mol and a molecular formula of C₂₂H₂₂O₁₀. It has a purity of 98%. It is a flavonoid glycoside. The compound should be stored under appropriate conditions, typically at -20°C, protected from light and moisture.
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| Toxicity/Toxicokinetics |
The toxicity profile of Swertisin is not extensively detailed. As a natural flavonoid, it is generally considered to have a good safety profile. However, comprehensive toxicological studies are required for therapeutic development. It is not intended for human therapeutic use without further development.
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| References |
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| Additional Infomation |
Swertisin is a flavonoid C-glycoside, a derivative of 7-O-methylapigenin, in which the hydrogen at the 6-position is replaced by a β-D-glucose residue. It is a plant metabolite with adenosine A1 receptor antagonist, anti-inflammatory, antioxidant, and hypoglycemic activity. It is a flavonoid C-glycoside, monosaccharide derivative, polyphenol, monomethoxyflavonoid, and dihydroxyflavonoid. Its function is related to that of apigenin. Swertisin has been reported to be found in columbine (Aquilegia oxysepala), gentian (Gentiana algida), and several other organisms with relevant data.
Swertisin is a C-glycosylflavone with anti-diabetic, antioxidant, and cognitive-enhancing properties. It is an oral adenosine A1 receptor antagonist and SGLT2 inhibitor. It is isolated from Swertia japonica and other medicinal plants. It is not approved for clinical use and is intended for research purposes only. |
| Molecular Formula |
C22H22O10
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|---|---|
| Molecular Weight |
446.4041
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| Exact Mass |
462.116
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| CAS # |
6991-10-2
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| PubChem CID |
124034
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| Appearance |
Light yellow to brown solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
798.1±60.0 °C at 760 mmHg
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| Flash Point |
279.7±26.4 °C
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| Vapour Pressure |
0.0±3.0 mmHg at 25°C
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| Index of Refraction |
1.695
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| LogP |
-1.03
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
705
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| Defined Atom Stereocenter Count |
5
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| SMILES |
COC1=C(C(=C2C(=C1)OC(=CC2=O)C3=CC=C(C=C3)O)O)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O
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| InChi Key |
ABRULANJVVJLFI-DGHBBABESA-N
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| InChi Code |
InChI=1S/C22H22O10/c1-30-13-7-14-16(11(25)6-12(31-14)9-2-4-10(24)5-3-9)19(27)17(13)22-21(29)20(28)18(26)15(8-23)32-22/h2-7,15,18,20-24,26-29H,8H2,1H3/t15-,18-,20+,21-,22+/m1/s1
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| Chemical Name |
5-hydroxy-2-(4-hydroxyphenyl)-7-methoxy-6-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]chromen-4-one
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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) |
DMSO : ~50 mg/mL (~112.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2401 mL | 11.2007 mL | 22.4014 mL | |
| 5 mM | 0.4480 mL | 2.2401 mL | 4.4803 mL | |
| 10 mM | 0.2240 mL | 1.1201 mL | 2.2401 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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