| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Tsugaric acid A acts on multiple pathways. It inhibits the activation of the STAT3 and NF-κB signaling pathways, leading to reduced expression of pro-inflammatory cytokines and anti-apoptotic proteins. It also suppresses the PI3K/Akt/mTOR pathway. The compound induces apoptosis by upregulating Bax and activating caspase-3 and caspase-9. Additionally, it has been reported to inhibit the growth of Gram-positive bacteria.
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| ln Vitro |
In vitro, tsugaric acid A inhibits the proliferation of human cancer cells, including HL-60 leukemia cells (IC50 ~ 7 µM) and A549 lung cancer cells (IC50 ~ 12 µM) after 48 hours. It reduces LPS-stimulated NO production in RAW 264.7 macrophages (IC50 ~ 5 µM). The compound shows antimicrobial activity against Staphylococcus aureus with an MIC of 16 µg/mL. It also exhibits weak antioxidant activity (DPPH IC50 ~ 45 µM).
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| ln Vivo |
In vivo, tsugaric acid A has shown anti-tumor effects in a mouse xenograft model using HL-60 cells. Intraperitoneal administration of 10 mg/kg every two days for 21 days resulted in a ~55% reduction in tumor volume. In a mouse model of LPS-induced acute lung injury, tsugaric acid A (5-15 mg/kg, i.p.) attenuated pulmonary inflammation and edema. It also showed protective effects in a mouse model of sepsis.
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| Enzyme Assay |
The in vitro STAT3 inhibition assay uses a luciferase reporter system. HeLa cells are co-transfected with STAT3-luciferase and Renilla reporter plasmids. After transfection, cells are treated with tsugaric acid A (1-20 µM) for 24 hours, then stimulated with IL-6 (50 ng/mL) for 6 hours. Luciferase activity is measured and normalized. The expression of STAT3 target genes (e.g., Bcl-xL, Survivin) is assessed by RT-qPCR and Western blotting.
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| Cell Assay |
For in vitro cytotoxicity assays, HL-60, A549, and normal human fibroblast cells are seeded in 96-well plates at 5 × 10³ cells/well. After overnight incubation, cells are treated with serial dilutions of tsugaric acid A (1-100 µM) for 24, 48, and 72 hours. Cell viability is measured using the MTT assay. Apoptosis is quantified by annexin V-FITC/PI staining and flow cytometry. Mitochondrial membrane potential is assessed using JC-1 staining.
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| Animal Protocol |
For in vivo xenograft studies, BALB/c nude mice (6-8 weeks, 18-22 g) are subcutaneously inoculated with 5 × 10⁶ HL-60 cells. When tumors reach ~100 mm³, mice are randomized into groups (n=8). Tsugaric acid A is dissolved in 10% DMSO/PBS and administered intraperitoneally at 5, 10, or 15 mg/kg every other day for 21 days. Tumor volumes and body weights are recorded. Tumors are excised and analyzed by Western blotting, TUNEL staining, and immunohistochemistry for proliferation markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of tsugaric acid A are limited. In rats, after intravenous administration (2 mg/kg), the half-life is approximately 2.8 hours. Oral bioavailability is low (<5%) due to poor absorption. The compound is highly lipophilic (Log P ~ 5.0) and exhibits high plasma protein binding (>90%). Metabolism is primarily via cytochrome P450, and excretion is via the biliary route.
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| Toxicity/Toxicokinetics |
Tsugaric acid A has low acute toxicity. The intraperitoneal LD50 in mice is approximately 100 mg/kg. At therapeutic doses (5-15 mg/kg), no significant organ toxicity is observed. The compound is not hemolytic at concentrations up to 100 µM. In a 14-day repeated dose study, doses of 20 mg/kg/day showed mild elevation of liver enzymes but no significant histopathological changes.
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| Additional Infomation |
Reports indicate that Ganoderma lucidum and Ganoderma lucidum contain tamarinic acid A, and relevant data is available for reference.
Tsugaric acid A is a white to light yellow powder. It is soluble in DMSO, ethanol, and methanol but insoluble in water. It is isolated from traditional Chinese medicinal plants used for treating inflammatory diseases and tumors. The compound is a research tool for studying the pharmacological effects of triterpenes. Its mechanism involves multiple pathways, including STAT3/NF-κB inhibition and apoptosis induction. |
| Molecular Formula |
C32H50O4
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|---|---|
| Molecular Weight |
498.7370
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| Exact Mass |
498.37
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| CAS # |
174391-64-1
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| PubChem CID |
71207558
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
577.3±50.0 °C at 760 mmHg
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| Melting Point |
181 - 182 °C
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| Flash Point |
174.4±23.6 °C
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| Vapour Pressure |
0.0±3.4 mmHg at 25°C
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| Index of Refraction |
1.536
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| LogP |
9.94
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
36
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| Complexity |
969
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=CCCC(C1CCC2(C1(CCC3=C2CCC4C3(CCC(C4(C)C)OC(=O)C)C)C)C)C(=O)O)C
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| InChi Key |
FIWGZIBLJWZUEA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H50O4/c1-20(2)10-9-11-22(28(34)35)23-14-18-32(8)25-12-13-26-29(4,5)27(36-21(3)33)16-17-30(26,6)24(25)15-19-31(23,32)7/h10,22-23,26-27H,9,11-19H2,1-8H3,(H,34,35)
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| Chemical Name |
2-(3-acetyloxy-4,4,10,13,14-pentamethyl-2,3,5,6,7,11,12,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-17-yl)-6-methylhept-5-enoic acid
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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 : ~10 mg/mL (~20.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.01 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (5.01 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 25.0 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 | 2.0051 mL | 10.0253 mL | 20.0505 mL | |
| 5 mM | 0.4010 mL | 2.0051 mL | 4.0101 mL | |
| 10 mM | 0.2005 mL | 1.0025 mL | 2.0051 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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