| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Astragaloside I targets the Wnt/β-catenin signaling pathway, stimulating osteoblast differentiation. It also activates the BMP pathway and RANK pathway. It inhibits the activation of BV-2 cells induced by LPS through suppressing the activation of PI3K/Akt/NF-κB pathway. This leads to the down-regulation of gene expressions of TNF-α, iNOS, and IL-1β.
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| ln Vitro |
In MC3T3-E1 cells, astragaloside I (10–40 μM) increases the expression of β-catenin, Runx2, BGP, and OPG, as well as RANKL (osteogenesis marker gene) [1].
In vitro, Astragaloside I stimulates osteoblast differentiation in MC3T3-E1 cells through the Wnt/β-catenin signaling pathway. It inhibits the activation of BV-2 cells induced by LPS by suppressing the PI3K/Akt/NF-κB pathway, reducing the nuclear translocation of phosphorylated NF-κB, and down-regulating the gene expressions of TNF-α, iNOS, and IL-1β. It also may protect cerebral tissue against free radical damage. |
| ln Vivo |
In vivo, Astragaloside I has been studied for its osteogenic properties. It may protect cerebral tissue against the free radical damage in ischemia. It has immunomodulatory, anti-inflammatory, antioxidant, and cardioprotective activities, with particular interest in immune regulation and cardiovascular health. It has demonstrated superior in vivo anti-fibrotic efficacy compared to astragaloside II and IV in a cholestatic liver disease model.
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| Enzyme Assay |
For cell-free assays, the Wnt/β-catenin pathway activation can be studied using reporter gene assays (e.g., TOPFlash/FOPFlash) with purified components. The inhibition of PI3K/Akt/NF-κB pathway can be assessed using kinase activity assays with purified PI3K, Akt, or IKK enzymes. The anti-inflammatory activity can be measured by assessing the inhibition of TNF-α, iNOS, and IL-1β production in cell-free systems.
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| Cell Assay |
Western blot analysis[1]
Cell Types: MC3T3-E1 cells. Tested Concentrations: 0, 10, 20, 40 μM. Incubation Duration: 5 days. Experimental Results: Stimulation of β-catenin and Runx2 expression. Cytotoxicity assay [1]. Cell Types: MC3T3-E1 cells. Tested Concentrations: 0, 10, 20, 40 μM. Incubation Duration: 1, 3 or 6 days (change medium every 2 days). Experimental Results: No obvious cytotoxic effect was found on MC3T3-E1 cells. For in vitro cellular assays, the osteogenic activity of Astragaloside I is assessed in MC3T3-E1 osteoblast precursor cells. Cells are treated with various concentrations of the compound, and osteoblast differentiation is assessed by measuring alkaline phosphatase (ALP) activity, mineralization (alizarin red staining), and expression of osteogenic markers (e.g., Runx2, Osterix) by qPCR or Western blot. Its anti-inflammatory activity is assessed in LPS-stimulated BV-2 microglial cells by measuring cytokine production and signaling pathway activation. |
| Animal Protocol |
For in vivo studies, Astragaloside I can be administered orally or intraperitoneally in animal models of bone disease (e.g., ovariectomized rats for osteoporosis), ischemia-reperfusion injury, or fibrosis. In bone disease models, endpoints include bone mineral density, bone volume, and histological analysis of bone tissue. In ischemia models, endpoints include infarct size, neurological deficit scores, and markers of oxidative stress. In fibrosis models, endpoints include fibrotic area and expression of fibrotic markers.
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| ADME/Pharmacokinetics |
Astragaloside I (CAS 84680-75-1) has a molecular formula of C45H72O16 and a molecular weight of 869.1 g/mol. It is also known as Astrasieversianin IV and Cyclosieversioside B. Purity is typically >98% for research use. Solubility: soluble in DMSO and other organic solvents. For in vitro studies, stock solutions are prepared in DMSO. For in vivo administration, it can be formulated in suitable vehicles. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a natural saponin from Astragalus membranaceus, it is generally considered to have low toxicity, but standard toxicological studies would be required for drug development. In vitro cytotoxicity assays in various cell lines are typically performed alongside efficacy studies to confirm that observed effects are not due to a general reduction in cell viability.
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| References | |
| Additional Infomation |
Astragaloside I is a research-grade compound and is not approved for therapeutic use. It serves primarily as a pharmacological tool for studying osteogenesis, Wnt/β-catenin signaling, and anti-inflammatory mechanisms. Its mechanism of action involves stimulating osteoblast differentiation through the Wnt/β-catenin pathway and inhibiting LPS-induced activation of BV-2 cells through the PI3K/Akt/NF-κB pathway. No clinical trials have been reported.
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| Molecular Formula |
C₄₅H₇₂O₁₆
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|---|---|
| Molecular Weight |
869.04
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| CAS # |
84680-75-1
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| PubChem CID |
13996685
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
910.6±65.0 °C at 760 mmHg
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| Flash Point |
265.5±27.8 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.603
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| LogP |
0.94
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
61
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| Complexity |
1690
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| Defined Atom Stereocenter Count |
21
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| Synonyms |
Cyclosieversioside B Astrasieversianin IV
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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 |
| 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 (~57.53 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (3.74 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 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 3.25 mg/mL (3.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1507 mL | 5.7535 mL | 11.5070 mL | |
| 5 mM | 0.2301 mL | 1.1507 mL | 2.3014 mL | |
| 10 mM | 0.1151 mL | 0.5753 mL | 1.1507 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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