| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Kauniolide targets multiple cellular pathways. It has been shown to inhibit the metabolism of cholesterol in cancer cells, leading to an increase in cellular cholesterol accumulation. It also blocks membrane transporters, inducing membrane accumulation of cholesterol and leading to cell death. Its anti-inflammatory effects are thought to be mediated through the inhibition of glucose-induced NF-κB activation, which is involved in diabetic neuropathy. Its anti-tumor activity is attributed to its cytotoxic effects, which are active against leukemia and breast cancer cells. Its stereoselective nature may play a role in its mechanism of action.
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| ln Vitro |
In vitro, Kauniolide displays significant inhibitory effects on the metabolism of cholesterol in cancer cells. It blocks membrane transporters and induces membrane accumulation of cholesterol, which leads to cell death. It has been shown to be active against leukemia and breast cancer cells. Its anti-inflammatory activity is evidenced by its potential to inhibit glucose-induced NF-κB activation. These diverse in vitro activities make it a valuable tool for studying cancer cell biology and inflammation.
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| ln Vivo |
In vivo activity data for Kauniolide is limited in publicly available literature. As a compound with potent anti-inflammatory, anti-tumor, and antimicrobial effects in vitro, it is hypothesized to exhibit similar effects in animal models. However, specific in vivo efficacy studies, including pharmacokinetic and pharmacodynamic parameters, have not been detailed in the available sources. Further research is needed to fully characterize its in vivo activity and therapeutic potential.
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| Enzyme Assay |
For cell-free enzyme assays, the ability of Kauniolide to block membrane transporters can be studied using transport assays with purified transporter proteins or membrane vesicles. The inhibition of cholesterol metabolism can be assessed in cell-free systems using microsomal preparations or purified enzymes involved in cholesterol synthesis and metabolism. The inhibition of NF-κB activation can be studied using cell-free transcription assays or by measuring the DNA-binding activity of NF-κB in nuclear extracts.
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| Cell Assay |
For in vitro cellular assays, the cytotoxic activity of Kauniolide is typically assessed in cancer cell lines, such as leukemia and breast cancer cells. Cells are seeded in multi-well plates and treated with varying concentrations of Kauniolide for a defined period (e.g., 48-72 hours). Cell viability is measured using MTT, MTS, or SRB assays, and the IC50 value is calculated. The effect on cholesterol metabolism can be studied by measuring the incorporation of radiolabeled acetate into cellular lipids or by measuring cellular cholesterol content using enzymatic assays. The induction of cell death can be assessed by flow cytometry using Annexin V/PI staining.
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| Animal Protocol |
For in vivo studies, Kauniolide could be administered orally or intraperitoneally in rodent models of cancer or inflammation. In a xenograft model, its anti-tumor efficacy would be assessed by measuring tumor volume over time. In a model of inflammation, such as carrageenan-induced paw edema, its anti-inflammatory effect would be assessed by measuring paw volume. Its effect on cholesterol metabolism could be studied in models of hypercholesterolemia.
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| ADME/Pharmacokinetics |
Kauniolide (C15H20O3) has a molecular weight of 248.32 g/mol. Its CAS number is 81066-45-7. It is typically supplied as a powder. It is soluble in organic solvents such as DMSO and ethanol. For in vitro studies, stock solutions are prepared in DMSO. For in vivo administration, it can be formulated in suitable vehicles. Storage is recommended at -20°C, protected from light. Its purity is typically >98% for research use.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available. As a sesquiterpene lactone, a class of compounds known for their diverse bioactivities, its safety profile would need to be established through standard toxicological studies. In vitro cytotoxicity assays in various cell lines are typically performed alongside efficacy studies to confirm that the observed effects are not due to a general reduction in cell viability.
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| Additional Infomation |
Reports indicate that Kauniolide is present in Critonia quadrangularis and Kaunia ignorata, and relevant data are available for reference.
Kauniolide is a research-grade compound and is not approved for any therapeutic use. It serves primarily as a valuable pharmacological tool for studying inflammation, cancer, and cholesterol metabolism. Its mechanism of action involves the modulation of various signaling pathways, the inhibition of cholesterol metabolism, and the blockade of membrane transporters. Its anti-tumor activity and its potential to inhibit NF-κB activation make it a compound of interest for drug discovery. No clinical trials have been reported. |
| Molecular Formula |
C15H18O2
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|---|---|
| Molecular Weight |
230.30222
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| Exact Mass |
230.131
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| CAS # |
81066-45-7
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| PubChem CID |
11791030
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| Appearance |
White to yellow solid powder
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| LogP |
3.16
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
17
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| Complexity |
467
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=C2CC=C([C@@H]2[C@@H]3[C@@H](CC1)C(=C)C(=O)O3)C
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| InChi Key |
AVLOGKPJWQCTLP-IHRRRGAJSA-N
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| InChi Code |
InChI=1S/C15H18O2/c1-8-4-7-12-10(3)15(16)17-14(12)13-9(2)5-6-11(8)13/h5,12-14H,3-4,6-7H2,1-2H3/t12-,13-,14-/m0/s1
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| Chemical Name |
(3aS,9aS,9bS)-6,9-dimethyl-3-methylidene-3a,4,5,7,9a,9b-hexahydroazuleno[4,5-b]furan-2-one
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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 (~434.22 mM)
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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 | 4.3422 mL | 21.7108 mL | 43.4216 mL | |
| 5 mM | 0.8684 mL | 4.3422 mL | 8.6843 mL | |
| 10 mM | 0.4342 mL | 2.1711 mL | 4.3422 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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