| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
Saikosaponin A targets multiple signaling pathways, including toll-like receptor 4 (TLR4), NF-κB, and MAPK pathways. It inhibits the activation of NF-κB and MAPKs (p38, ERK, JNK), thereby suppressing the production of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6. Saikosaponin A also modulates the expression of TLR4 and inhibits lipopolysaccharide (LPS)-induced inflammatory responses. Additionally, it induces apoptosis in cancer cells by activating caspase cascades and modulating Bcl-2 family proteins.
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| ln Vitro |
Human osteoarthritis nurse cells have no effect on the viability of saikosaponin A (5–15 μM, 24 hours) [1]. Saikosaponin A (5-15 μM, 24 h) increases the expression of LXRα in a dose-dependent manner and suppresses the generation of NO, PGE2, and NF-κB produced by IL-1β [1].
In vitro, saikosaponin A exhibits potent anti-inflammatory activity by inhibiting LPS-induced nitric oxide (NO) production and iNOS expression in macrophages. It suppresses the secretion of TNF-α, IL-6, and IL-1β in various cell types. Saikosaponin A also shows antiviral activity against influenza virus and hepatitis B virus by inhibiting viral replication. It induces apoptosis in hepatocellular carcinoma cells and other cancer cell lines, with IC50 values in the micromolar range. Its hepatoprotective effects are demonstrated in cultured hepatocytes against toxic insults. |
| ln Vivo |
Saikosaponin A (1-10 mg/kg, intraperitoneal injection, 7 days) can stop the morphological alterations brought on by 5-FU in the small intestine. [2]. Saikosaponin-A (1–10 mg/kg, intraperitoneal, 7 days) improves 5-FU-induced mucositis in 5
In vivo, saikosaponin A has demonstrated significant hepatoprotective effects in animal models of liver injury induced by carbon tetrachloride, acetaminophen, or alcohol. It reduces serum transaminase levels, improves histopathological changes, and decreases oxidative stress markers in the liver. Saikosaponin A also exhibits anti-inflammatory effects in models of colitis and arthritis, and antiviral efficacy in influenza-infected mice. Its anticancer activity has been shown in xenograft models, where it inhibits tumor growth and metastasis. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for saikosaponin A are not typically performed because the compound modulates signaling pathways rather than directly binding to a single enzyme. However, its inhibitory effects on NF-κB activation can be assessed using electrophoretic mobility shift assays (EMSA) or luciferase reporter assays with NF-κB-responsive plasmids. Kinase activity assays can measure the inhibition of MAPKs (p38, ERK, JNK) using recombinant proteins and specific substrates. TLR4 binding can be evaluated using surface plasmon resonance.
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| Cell Assay |
Western Blot Analysis
Cell Types: Human Osteoarthritis Chondrocytes Tested Concentrations: 5, 10, 15 μM Incubation Duration: 24. h Experimental Results: Inhibition of IL-1β-induced NF-κB p65 and IκBα phosphorylation levels. Upregulates the expression of LXRα in a dose-dependent manner. In vitro cellular assays for saikosaponin A are performed using macrophages (e.g., RAW264.7), hepatocytes (e.g., HepG2), and cancer cell lines. Cells are treated with varying concentrations of saikosaponin A, then stimulated with LPS or other inflammatory agents. Nitric oxide production is measured using Griess reagent. Cytokine levels are quantified by ELISA. Cell viability is assessed by MTT assays. Apoptosis is evaluated by annexin V staining and caspase activity assays. Western blotting is used to detect changes in signaling proteins like NF-κB and MAPKs. |
| Animal Protocol |
Animal/Disease Models: BALB/c mouse model [2]
Doses: 1, 5, 10 mg /kg/day, 7 d Route of Administration: intraperitoneal (ip) injection Experimental Results: diminished villous blunting, crypt cell apoptosis and inflammatory cell infiltration. The concentrations of GSH, GST, catalase and SOD in intestinal tissue were diminished. In vivo animal experiments for saikosaponin A are conducted in rodent models of liver injury, inflammation, and cancer. For hepatoprotection, mice or rats are administered saikosaponin A orally or intraperitoneally prior to CCl4 or acetaminophen challenge, and serum ALT/AST levels, liver histology, and oxidative stress markers are measured. In inflammation models, paw edema or colitis severity is assessed. Anticancer efficacy is evaluated in xenograft mice by measuring tumor volume and weight after treatment with saikosaponin A. |
| ADME/Pharmacokinetics |
Saikosaponin A has a molecular weight of 780.99 g/mol and a molecular formula of C42H68O13. It is a white to off-white powder, soluble in DMSO and ethanol, but poorly soluble in water. The compound has moderate oral bioavailability and undergoes extensive metabolism in the liver. Its half-life in rats is approximately 2-4 hours after intravenous administration. Saikosaponin A is primarily excreted via bile and feces. Pharmacokinetic studies in humans are limited due to its research status.
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| Toxicity/Toxicokinetics |
Saikosaponin A has been evaluated for safety in preclinical studies. The compound is well-tolerated at therapeutic doses, with no significant acute toxicity observed in mice at oral doses up to 1000 mg/kg. Chronic toxicity studies are limited, but hepatotoxicity has been reported at very high doses. Saikosaponin A can cause hemolysis due to its saponin structure, so caution is needed for intravenous administration. It is considered safe for research purposes but requires further toxicological evaluation.
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| References | |
| Additional Infomation |
Saikosaponin A is a saikosaponin. It has been reported that saikosaponin A exists in Bupleurum chinense, Scrophularia ningpoensis, and other organisms with relevant data.
Saikosaponin A is a major bioactive component of Bupleurum species, used in traditional Chinese medicine to treat liver disorders and inflammatory diseases. Its mechanism involves inhibition of TLR4, NF-κB, and MAPK pathways, leading to reduced inflammation and apoptosis. Saikosaponin A has shown promise in preclinical studies for hepatitis, liver fibrosis, cancer, and viral infections. However, it is not an approved drug and remains a research compound. Its saponin nature limits oral bioavailability, prompting interest in structural modification and formulation development. |
| Molecular Formula |
C42H68O13
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| Molecular Weight |
780.99
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| Exact Mass |
780.466
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| CAS # |
20736-09-8
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| Related CAS # |
20736-09-8;
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| PubChem CID |
167928
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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 |
893.7±65.0 °C at 760 mmHg
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| Melting Point |
225 - 235ºC
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| Flash Point |
494.3±34.3 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.617
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| LogP |
3.65
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
55
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| Complexity |
1490
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| Defined Atom Stereocenter Count |
21
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| SMILES |
C[C@@H]1[C@@H]([C@@H]([C@H]([C@@H](O1)O[C@H]2CC[C@]3([C@H]([C@]2(C)CO)CC[C@@]4([C@@H]3C=C[C@@]56[C@]4(C[C@@H]([C@@]7([C@H]5CC(CC7)(C)C)CO6)O)C)C)C)O)O[C@H]8[C@@H]([C@H]([C@@H]([C@H](O8)CO)O)O)O)O
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| InChi Key |
KYWSCMDFVARMPN-MSSMMRRTSA-N
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| InChi Code |
InChI=1S/C42H68O13/c1-21-28(46)33(55-34-31(49)30(48)29(47)22(18-43)53-34)32(50)35(52-21)54-27-10-11-37(4)23(38(27,5)19-44)8-12-39(6)24(37)9-13-42-25-16-36(2,3)14-15-41(25,20-51-42)26(45)17-40(39,42)7/h9,13,21-35,43-50H,8,10-12,14-20H2,1-7H3/t21-,22-,23-,24-,25-,26+,27+,28+,29-,30+,31-,32-,33+,34+,35+,37+,38+,39-,40+,41-,42+/m1/s1
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| Chemical Name |
(2S,3R,4S,5S,6R)-2-[(2R,3R,4S,5S,6R)-3,5-dihydroxy-2-[[(1S,2S,4S,5R,8R,9R,10S,13S,14R,17S,18R)-2-hydroxy-9-(hydroxymethyl)-4,5,9,13,20,20-hexamethyl-24-oxahexacyclo[15.5.2.01,18.04,17.05,14.08,13]tetracos-15-en-10-yl]oxy]-6-methyloxan-4-yl]oxy-6-(hydroxymethyl)oxane-3,4,5-triol
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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 : ~100 mg/mL (~128.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.20 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 (3.20 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 (3.20 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 | 1.2804 mL | 6.4021 mL | 12.8043 mL | |
| 5 mM | 0.2561 mL | 1.2804 mL | 2.5609 mL | |
| 10 mM | 0.1280 mL | 0.6402 mL | 1.2804 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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