| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Esculentoside A targets cyclooxygenase-2 (COX-2) with selective inhibitory activity. It also targets the nuclear factor kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways, suppressing inflammatory responses. The compound modulates T cell-mediated adaptive immunity, suggesting potential applications in autoimmune diseases. Its anti-inflammatory activity is mediated through inhibition of these key inflammatory signaling pathways, making it a valuable tool for studying inflammation and immune regulation.
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| ln Vitro |
Sensitized macrophages release less TNF when exposed to EscuLentoside A (0-10 μM; 24) [4].
In vitro studies have demonstrated that Esculentoside A possesses significant anti-inflammatory activity. It exhibits selective inhibitory activity towards cyclooxygenase-2 (COX-2). The compound suppresses inflammatory responses through inhibition of the NF-κB and MAPK signaling pathways. Esculentoside A also shows potential anticancer and antioxidant properties. Its ability to modulate T cell-mediated adaptive immunity suggests applications in autoimmune disease research. However, detailed in vitro potency data (e.g., IC₅₀ values for COX-2 inhibition) are limited in the published literature. |
| ln Vivo |
EscuLentoside A (EsA) (intraperitoneal injection; 5, 10, and 20 mg/kg; once daily; 7 days) dose induces reduction in serum TNF, IL-1, and IL-6 levels in mice following LPS challenge. EscuLentoside A (EsA) (ip; 20 mg/kg; once daily; 4 weeks) plays an important role in the management of BXSB by modulating inflammatory cytokines, inhibiting renal cell proliferation, and inducing cytokines [2].
In vivo, Esculentoside A has been shown to suppress inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the NF-κB and MAPK signaling pathways. It possesses anti-inflammatory activity in acute and chronic experimental models. The compound may be useful for the treatment of autoimmune disease through modulation of T cell-mediated adaptive immunity. These findings suggest that Esculentoside A has potential therapeutic applications in inflammatory and autoimmune diseases. |
| Enzyme Assay |
In vitro non-cell enzyme assays for Esculentoside A typically involve measuring COX-2 inhibition using purified COX-2 enzyme. The compound is incubated with COX-2 enzyme and arachidonic acid substrate, and prostaglandin production is measured by ELISA or radiometric methods. IC₅₀ values are calculated from dose-response curves. Kinase inhibition assays can be performed to evaluate the compound's effects on MAPK signaling components (e.g., p38, JNK, ERK) using purified kinases and peptide substrates.
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| Cell Assay |
In vitro cell-based assays for Esculentoside A use macrophages, immune cells, or other relevant cell lines stimulated with LPS to induce inflammatory responses. Cells are treated with Esculentoside A at various concentrations, and parameters such as inflammatory cytokine production (TNF-α, IL-6, IL-1β) are measured by ELISA. NF-κB and MAPK activation are assessed by Western blotting using phospho-specific antibodies (e.g., p-p38, p-JNK, p-ERK, p-IκBα). Cell viability is assessed using MTT or CCK-8 assays to evaluate cytotoxicity.
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| Animal Protocol |
Animal/Disease Models: BXSB mice [ 2]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection; [4]. 20 mg/kg; one time/day; 4 weeks Experimental Results: Reduces renal damage in LN. In vivo animal studies for Esculentoside A employ rodent models of acute lung injury (ALI) induced by LPS. The compound is administered via intraperitoneal or intravenous injection, and parameters assessed include lung histopathology, inflammatory cell infiltration, cytokine levels in bronchoalveolar lavage fluid (BALF), and activation of NF-κB and MAPK signaling pathways in lung tissues. Other models of inflammation (e.g., carrageenan-induced paw edema) and autoimmune disease may also be used to evaluate the compound's efficacy. |
| ADME/Pharmacokinetics |
Esculentoside A has a molecular weight of approximately 827 g/mol and a molecular formula of C₄₂H₆₆O₁₆. It is a triterpenoid saponin with a complex glycosidic structure. The compound should be stored at -20°C. It is soluble in organic solvents such as DMSO. Due to its high molecular weight and saponin structure, Esculentoside A is expected to have poor oral bioavailability. Detailed pharmacokinetic parameters have not been extensively characterized.
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| Toxicity/Toxicokinetics |
The toxicity profile of Esculentoside A has not been comprehensively evaluated in published studies. As a natural component of Phytolacca esculenta, which has been used in traditional medicine, it is generally considered to have low toxicity at therapeutic doses. However, saponins can have hemolytic activity and may cause gastrointestinal irritation at high doses. The compound is classified as a research reagent and is not intended for human therapeutic use. Comprehensive toxicological studies have not been reported.
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| References |
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| Additional Infomation |
Esculentoside A is a triterpenoid saponin derived from the root of Phytolacca esculenta (Chinese pokeweed). It is also known as 商陆皂苷甲 in Chinese. The compound exhibits selective COX-2 inhibitory activity and suppresses inflammatory responses through inhibition of the NF-κB and MAPK signaling pathways. It may be useful for the treatment of autoimmune disease through modulation of T cell-mediated adaptive immunity. Not approved for clinical use; intended for research purposes only.
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| Molecular Formula |
C42H66O16
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| Molecular Weight |
826.963840000001
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| Exact Mass |
826.435
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| CAS # |
65497-07-6
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| Related CAS # |
Esculentoside A; 65497-07-6
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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 |
935.8±65.0 °C at 760 mmHg
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| Flash Point |
275.1±27.8 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.620
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| Source |
Originated from plants: Phytolaccaceae Phytolacca acinosa Roxb.
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| LogP |
3.01
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| SMILES |
C[C@@]1(CC[C@]2(C(O)=O)[C@@]3([H])C[C@](C(OC)=O)(C)CC2)C3=CC[C@@]4([H])[C@]1(CC[C@]5([H])[C@@]4(C[C@H](O)[C@H](O[C@@](OC[C@@H](O[C@]([C@@H]([C@@H](O)[C@@H]6O)O)([H])O[C@@H]6CO)[C@@H]7O)([H])[C@@H]7O)[C@@]5(C)CO)C)C
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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 : ~100 mg/mL (~120.92 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.02 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 25.0 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: ≥ 2.5 mg/mL (3.02 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 25.0 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: ≥ 2.5 mg/mL (3.02 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 | 1.2092 mL | 6.0462 mL | 12.0925 mL | |
| 5 mM | 0.2418 mL | 1.2092 mL | 2.4185 mL | |
| 10 mM | 0.1209 mL | 0.6046 mL | 1.2092 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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