| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Aescin A (24 h) dose-dependently inhibited cholesterol ester accumulation induced by acetylated low-density lipoprotein (ACD) in human monocyte-derived macrophages (but not triglyceride accumulation) and did not induce cytotoxicity [2]. Aescin A (5 h) did not inhibit the binding or degradation of acetylated low-density lipoprotein (ACD) in human monocyte-derived macrophages [2]. Aescin A (24 h) dose-dependently inhibited cholesterol ester accumulation in Chinese hamster ovary cells overexpressing human ACAT-1 or human ACAT-2 and did not induce cytotoxicity [2]. Aescin A (15 min) dose-dependently inhibited ACAT activity in microsomes of human monocyte-derived macrophages, Chinese hamster ovary cells overexpressing human ACAT-1, and Chinese hamster ovary cells overexpressing human ACAT-2, with 50 μmol/L of aescin A inhibiting ACAT activity in HMDM by up to 40% [2]. Aescin A (24 h) dose-dependently reduced the expression of ACAT-1 protein in human monocyte-derived macrophages without affecting the expression of SR-A or SR-BI [2]. Aescin A (10-100 μM; 24 h) dose-dependently and potently inhibited the accumulation of cholesterol esters in human monocyte-derived macrophages (HMDM) without affecting the uptake or degradation of acetyl-LDL, with 50 μM of aescin A reducing cholesterol ester accumulation by up to 40% [3]. Aescin A (10-100 μM; 24 h) dose-dependently inhibited the accumulation of cholesterol esters in hACAT-1 CHO cells and hACAT-2 CHO cells [3]. Aescin A (10-100 μM) dose-dependently inhibited ACAT activity in human monocyte-derived macrophages (HMDM), hACAT-1 CHO cells and hACAT-2 CHO cells [3]. Aescin A (10-50 μM; 24 h) dose-dependently reduced the expression of ACAT-1 protein in human monocyte-derived macrophages (HMDM) without altering the expression of SR-A or SR-BI [3].
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|---|---|
| ln Vivo |
Escolucoside A (50-200 mg/kg; orally; once daily; for 12 weeks) can dose-dependently alleviate non-alcoholic fatty liver disease in rats fed a high-fat diet. Its mechanism of action includes normalizing liver enzyme and lipid levels, improving liver histology, activating the Nrf2 antioxidant pathway, inhibiting NF-κB-mediated inflammation, and regulating hepatic lipogenesis and fatty acid oxidation. The 200 mg/kg dose can completely restore most indicators to control levels [1]. Escolucoside A (100 mg/kg/day; orally; once daily; for 90 days) is produced in vivo by oral administration of escolucoside A and can be detected in the aorta of apolipoprotein E-deficient mice [3].
|
| Cell Assay |
Western Blot Analysis [3]
Cell Types: Human monocyte-derived macrophages (HMDM) Tested Concentrations: 10, 30, 50 μM Incubation Duration: 24 hours Experimental Results: ACAT-1 protein expression in HMDM decreased in a dose-dependent manner. SR-A and SR-BI protein expression remained unchanged compared to the control group. |
| Animal Protocol |
Animal/Disease Models:Wistar (male, 10-11 weeks old, initial weight approximately 165 g, induced by a high-fat diet) [1]
Doses: 50 mg/kg; 100 mg/kg; 200 mg/kg Route of Administration: Oral; Daily; 12 weeks Experimental Results: Dose-dependently reduced serum ALT, AST, GGT, serum/liver TG, CHOL, LDL-c, liver weight/liver to body weight ratio, NF-κB nuclear activity, IKKβ activity, liver MDA, IL-6, TNF-α, and liver SREBP1, ACC mRNA. Dose-dependently increased liver Nrf2 (mRNA, cytoplasm, nucleus), GSH, SOD, CAT, HO-1, and liver PPARα, CPT I mRNA. Dose-dependently reduced hepatocyte fat vacuoles and improved liver structure. A dose of 200 mg/kg reduced serum/liver triglyceride (TG), cholesterol (CHOL), and serum low-density lipoprotein cholesterol (LDL-c) levels in normally fed rats without adverse effects on body weight, fat pad weight, or glucose/insulin parameters. Animal/Disease Models:C57BL/6.KOR-Apoeshl (apoE-deficient) [2] Doses: 50 mg/kg/day; 100 mg/kg/day (administered as esculeoside A, converted to esculeogenin A in vivo) Route of Administration: Oral; daily; 90 days Experimental Results: Serum total cholesterol decreased by approximately 25%, serum low-density lipoprotein cholesterol decreased by approximately 25%, and serum triglycerides decreased by approximately 45%. Atherosclerotic lesions on the aortic surface decreased to 8.2%. The lesion area in the aortic sinus cross section decreased by 52%. Esculeoogenin A was detected in the aorta of treated mice, confirming the conversion of esculeoside A in vivo. |
| References |
| Molecular Formula |
C27H45NO4
|
|---|---|
| Molecular Weight |
447.65
|
| CAS # |
854381-37-6
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
C[C@@H]1[C@@]2([C@@H](C[C@@H](CN2)CO)O)O[C@]3([H])[C@@]1([H])[C@@]4([C@@]([C@@]5([H])[C@]([C@@]6([C@@](C[C@H](CC6)O)([H])CC5)C)([H])CC4)([H])C3)C
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 2.2339 mL | 11.1694 mL | 22.3389 mL | |
| 5 mM | 0.4468 mL | 2.2339 mL | 4.4678 mL | |
| 10 mM | 0.2234 mL | 1.1169 mL | 2.2339 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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