| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Tussilagone has multiple molecular targets, with its primary mechanism involving the induction of heme oxygenase-1 (HO-1). It is an effective HO-1 inducer, which mediates its anti-inflammatory effects. Tussilagone also inhibits NF-κB signaling and the production of pro-inflammatory cytokines. It has been shown to inhibit VEGFR2 signaling, which contributes to its anti-angiogenic activity.
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| ln Vitro |
In lipopolysaccharide-stimulated RAW 264.7 cells and the peritoneum, tussilagone suppresses the expression of inflammatory mediators such as nitric oxide and prostaglandin E2, as well as inflammatory cytokines such as tumor necrosis factor-alpha (TNF-alpha) and high mobility group box 1 (HMGB1). Phagocytosis. Additionally, tussilagone lessens the activation of nuclear factor kappa light chain enhancer of activated B cells (NF-κB) and mitogen-activated protein kinase, which are involved in the activation of several inflammatory mediators in activated macrophages [1].
In vitro, tussilagone has demonstrated significant anti-inflammatory activity. It inhibits the overproduction of nitric oxide and prostaglandin E2 in BV-2 microglia, with IC50 values of 8.67 µM for NO inhibition and 14.1 µM for PGE2 inhibition. It also inhibits dendritic cell function. These activities are mediated through the induction of HO-1 and the suppression of NF-κB signaling. |
| ln Vivo |
In mice with CLP-activated sepsis, tussilagone treatment (1 mg/kg and 10 mg/kg) decreased lung damage and mortality. An injection of tussilagone can reduce the increased production of TNF-α and cyclooxygenase (COX)-2 in the alveolar macrophages of septic mice [2].
In vivo, tussilagone has shown protective effects in several animal models. It ameliorates inflammatory responses in dextran sulphate sodium-induced murine colitis. It also inhibits the inflammatory response and improves survival in cecal ligation and puncture (CLP)-induced septic mice. These effects are consistent with its anti-inflammatory and immunomodulatory properties. |
| Enzyme Assay |
In vitro enzyme or receptor binding (non-cell) assays for tussilagone involve studying its ability to induce HO-1 activity. This can be measured using a biochemical assay where the enzyme activity is monitored in cell lysates. Its inhibition of NF-κB activation can be assessed using an electrophoretic mobility shift assay (EMSA) with a labeled NF-κB DNA probe.
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| Cell Assay |
In vitro cell-based assays for tussilagone are performed using immune cells like dendritic cells or macrophages. Cells are treated with the compound and then stimulated with LPS or other inflammatory agents. The production of pro-inflammatory cytokines (e.g., TNF-α, IL-6) is measured using ELISA. HO-1 protein levels are assessed by Western blotting. The compound's ability to inhibit NO production is measured using the Griess assay.
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| Animal Protocol |
In vivo animal experiments for tussilagone are conducted using mouse models of inflammation and sepsis. In the colitis model, mice are treated with dextran sulphate sodium in drinking water to induce colitis, followed by oral or intraperitoneal administration of tussilagone. Colon tissues are collected for histological analysis and cytokine measurement. In the sepsis model, mice undergo cecal ligation and puncture (CLP), and survival is monitored.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of tussilagone have been studied to support its use as a research compound. As a sesquiterpene, it is lipophilic and is expected to be well-absorbed after oral administration. Its half-life and bioavailability are determined in preclinical studies via LC-MS/MS analysis of plasma samples.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for tussilagone are limited. As a natural product, it is generally considered safe at moderate doses. However, its safety profile requires thorough evaluation in long-term toxicology studies, particularly given its potential effects on the immune system.
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| References |
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| Additional Infomation |
Unii-95N0gbb2SX has been reported in Parasenecio petasitoides and Tussilago farfara, with available data. See also: Tussilago farfara flowers (partial); Tussilago farfara leaves (partial).
Other information: Tussilagone is a pharmacopoeia quality marker for Farfarae Flos (coltsfoot flower). It has been studied for its potential therapeutic applications in respiratory, neurological, and cardiovascular health. The compound is available as a research reagent for preclinical studies. |
| Molecular Formula |
C23H34O5
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|---|---|
| Molecular Weight |
390.52
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| Exact Mass |
390.24
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| CAS # |
104012-37-5
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| PubChem CID |
13919185
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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 |
471.3±35.0 °C at 760 mmHg
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| Flash Point |
200.7±26.0 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.502
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| LogP |
5.03
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
28
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| Complexity |
675
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC/C(=C/C(=O)O[C@@H]1C[C@H]([C@H]2[C@H](C1=C)CC(=O)[C@@H]2[C@@H](C)OC(=O)C)C(C)C)/C
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| InChi Key |
CFUPNMDNSQIWBB-UUVDBSHOSA-N
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| InChi Code |
InChI=1S/C23H34O5/c1-8-13(4)9-21(26)28-20-11-17(12(2)3)23-18(14(20)5)10-19(25)22(23)15(6)27-16(7)24/h9,12,15,17-18,20,22-23H,5,8,10-11H2,1-4,6-7H3/b13-9+/t15-,17+,18+,20-,22+,23+/m1/s1
|
| Chemical Name |
[(1S,3aR,5R,7S,7aS)-1-[(1R)-1-acetyloxyethyl]-4-methylidene-2-oxo-7-propan-2-yl-3,3a,5,6,7,7a-hexahydro-1H-inden-5-yl] (E)-3-methylpent-2-enoate
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| Synonyms |
L 652469; L-652469; Tussilagone
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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 : ~62.5 mg/mL (~160.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (16.00 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 62.5 mg/mL clear DMSO stock solution to 900 μL 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 | 2.5607 mL | 12.8034 mL | 25.6069 mL | |
| 5 mM | 0.5121 mL | 2.5607 mL | 5.1214 mL | |
| 10 mM | 0.2561 mL | 1.2803 mL | 2.5607 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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