| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Swertiamarin targets multiple pathways including MMP, NF-κB, JAK, and Keap1-Nrf2. It inhibits HMG-CoA reductase activity, making it a potential antiatherogenic agent. It also modulates the dopamine D2 receptor to stimulate gastric emptying and small intestinal motility.
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|---|---|
| ln Vitro |
In vitro, swertiamarin (50 μg/mL) inhibits nitric oxide (NO) production in IL-1β-stimulated fibroblast-like synoviocytes (FLSs) isolated from rat hindpaw. It regulates the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promotes osteoblast proliferation. It possesses antioxidant and hepatoprotective effects.
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| ln Vivo |
In vivo, swertiamarin exhibits anti-hyperglycemic, anti-hyperlipidemic, and anti-diabetic activity, enhancing β cell regeneration which causes reversal of diabetes. It acts as an anti-rheumatic agent by modulating NF-κB/IκB and JAK2/STAT3 signaling. It has shown potential as an antiatherogenic agent by inhibiting HMG-CoA reductase activity in high cholesterol-fed rats.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays typically involve evaluating swertiamarin's inhibitory activity against HMG-CoA reductase or its binding affinity to the dopamine D2 receptor. IC50 or Ki values are determined using radioligand binding or enzymatic activity assays.
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| Cell Assay |
For in vitro cell-based assays, swertiamarin is dissolved in DMSO (64 mg/mL; 170.97 mM) and applied to cultured cells such as fibroblast-like synoviocytes or osteoblasts at concentrations ranging from 10-100 μg/mL. Effects on NO production, cytokine levels, or cell proliferation are typically assessed after 24-48 hours of treatment.
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| Animal Protocol |
In vivo animal studies commonly use rat models. Swertiamarin is administered orally or intraperitoneally at doses ranging from 10-100 mg/kg. Efficacy is evaluated by measuring blood glucose, lipid profiles, inflammatory markers, and histopathological examination of tissues such as the liver and joints.
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| ADME/Pharmacokinetics |
Swertiamarin is orally active with good bioavailability. It is soluble in DMSO (64 mg/mL; 170.97 mM). As a glycoside, it may undergo deglycosylation in vivo to active metabolites such as genitianine, which upregulates PPAR-γ gene expression.
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| Toxicity/Toxicokinetics |
Swertiamarin has a low toxicity profile and is considered safe for research use. It has shown hepatoprotective effects against carbon tetrachloride-induced liver toxicity in rats through the Nrf2/HO-1 pathway. No significant acute toxicity has been reported at therapeutic doses.
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| References | |
| Additional Infomation |
Swertiamarin is a glycoside. It has been reported to exist in Schultesia lisianthoides, Gentiana thunbergii, and other organisms with relevant data. See also: whole plant (part) of Centaurium erythraea.
Swertiamarin is used in traditional medicine for the treatment of diabetes and arthritis. It has cardioprotective and anti-atherosclerotic effects, and stimulates gastric emptying by inhibiting the dopamine D2 receptor, making it a potential remedy for functional dyspepsia. It also exhibits immunomodulatory activity. |
| Molecular Formula |
C16H22O10
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|---|---|
| Molecular Weight |
374.342
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| Exact Mass |
374.121
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| CAS # |
17388-39-5
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| PubChem CID |
442435
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
649.3±55.0 °C at 760 mmHg
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| Melting Point |
111ºC
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| Flash Point |
237.7±25.0 °C
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| Vapour Pressure |
0.0±4.4 mmHg at 25°C
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| Index of Refraction |
1.626
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| LogP |
-3.15
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
592
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
C=C[C@H]1[C@@H](OC=C2[C@]1(CCOC2=O)O)O[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O
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| InChi Key |
HEYZWPRKKUGDCR-QBXMEVCASA-N
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| InChi Code |
InChI=1S/C16H22O10/c1-2-7-14(24-6-8-13(21)23-4-3-16(7,8)22)26-15-12(20)11(19)10(18)9(5-17)25-15/h2,6-7,9-12,14-15,17-20,22H,1,3-5H2/t7-,9+,10+,11-,12+,14-,15-,16+/m0/s1
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| Chemical Name |
(3S,4R,4aR)-4-ethenyl-4a-hydroxy-3-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3,4,5,6-tetrahydropyrano[3,4-c]pyran-8-one
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| Synonyms |
Swertiamaroside Swertiamarin
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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 : ~250 mg/mL (~667.84 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.17 mg/mL (5.80 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 21.7 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: ≥ 2.17 mg/mL (5.80 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 21.7 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: ≥ 2.17 mg/mL (5.80 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 | 2.6714 mL | 13.3568 mL | 26.7137 mL | |
| 5 mM | 0.5343 mL | 2.6714 mL | 5.3427 mL | |
| 10 mM | 0.2671 mL | 1.3357 mL | 2.6714 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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