| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
miR-34a, Notch-1 [2]
Acetylcholine receptor, histamine receptor (related to ileal smooth muscle contraction) [1] |
|---|---|
| ln Vitro |
Cirsiliol causes concentration-dependent relaxation in the isolated rat ileum at concentrations ranging from 0.01 to 300 μM. Cirsiliol may promote the release of intracellularly stored Ca2+ while inhibiting Ca2+ influx[1]. By blocking radiation-induced Notch-1 expression, rhamnetin or cirsiliol treatment inhibits the proliferation of NSCLC cells [2].
- Cirsiliol (1-100 μM) dose-dependently inhibited acetylcholine and histamine-induced contraction of isolated rat ileum. At 100 μM, it achieved a maximal inhibition rate of ~70% for acetylcholine-induced contraction and ~65% for histamine-induced contraction (detected by isometric tension measurement) [1] - In non-small cell lung cancer (NSCLC) cell lines (A549, H1299), Cirsiliol (5, 10, 20 μM) enhanced radiosensitivity. When combined with ionizing radiation (2-8 Gy), it reduced cell viability (MTT assay) and increased apoptotic rate (Annexin V-FITC/PI staining) compared with radiation alone [2] - Cirsiliol (5-20 μM) suppressed epithelial-mesenchymal transition (EMT) in NSCLC cells: upregulated epithelial marker E-cadherin and downregulated mesenchymal markers N-cadherin and vimentin (Western blot) [2] - Cirsiliol (5-20 μM) upregulated miR-34a expression (qPCR) and downregulated Notch-1 mRNA and protein expression (qPCR, Western blot) in NSCLC cells, mediating its radiosensitizing and EMT-inhibiting effects [2] - Cirsiliol (10, 20 μM) dose-dependently reduced the migration and invasion of A549 and H1299 cells (Transwell assay) [2] |
| ln Vivo |
In comparison to radiation alone, combination treatment with rhamnetin or cecillin significantly reduced the tumor volume in xenograft mice models [2].
|
| Enzyme Assay |
- Isolated ileum contraction assay: Rat ileum segments (2-3 mm) were mounted in organ baths with oxygenated Krebs solution (37°C, pH 7.4) and connected to force transducers. After 60-minute equilibration, segments were contracted with acetylcholine (1 μM) or histamine (10 μM). Cirsiliol (1-100 μM) was added cumulatively, and isometric tension changes were recorded to construct concentration-response curves and calculate inhibition rates [1]
|
| Cell Assay |
- NSCLC cell radiosensitivity assay: A549/H1299 cells were seeded in 96-well plates, pretreated with Cirsiliol (5-20 μM) for 24 hours, then exposed to 2-8 Gy ionizing radiation. Cell viability was detected by MTT assay 48 hours post-radiation; apoptotic rate was measured by Annexin V-FITC/PI staining and flow cytometry [2]
- EMT and pathway analysis: NSCLC cells were treated with Cirsiliol (5-20 μM) for 48 hours. Total RNA was extracted for qPCR to detect miR-34a and Notch-1 mRNA expression (GAPDH as internal control). Proteins were extracted for Western blot to analyze Notch-1, E-cadherin, N-cadherin, vimentin, and β-actin levels [2] - Migration and invasion assay: NSCLC cells were treated with Cirsiliol (10, 20 μM) for 24 hours, then seeded in Transwell upper chambers (with Matrigel for invasion assay). After 24-48 hours incubation, migrated/invasive cells in the lower chamber were stained and counted [2] |
| References |
|
| Additional Infomation |
Cirsiliol is a dimethoxyflavonoid with a flavonoid structure, where methoxy groups are substituted at the 6 and 7 positions, and hydroxyl groups are substituted at the 5, 3', and 4' positions. It is a plant metabolite. It is a trihydroxyflavonoid and a dimethoxyflavonoid. Its function is related to flavonoid compounds. Cirsiliol has been reported to be found in yarrow (Achillea setacea), sage (Salvia officinalis), and other organisms with relevant data.
- Cirsiliol is a natural flavonoid compound isolated from the herb Achillea fragrantissima [1][2] - Its core biological mechanisms include: inhibiting acetylcholine/histamine-mediated ileal smooth muscle contraction [1]; enhancing the radiosensitivity of non-small cell lung cancer cells and inhibiting EMT by regulating the miR-34a/Notch-1 signaling pathway [2] - Cirsiliol has potential application value as a non-small cell lung cancer radiosensitizer and intestinal smooth muscle function modulator [1][2] |
| Molecular Formula |
C17H14O7
|
|---|---|
| Molecular Weight |
330.28886
|
| Exact Mass |
330.073
|
| CAS # |
34334-69-5
|
| PubChem CID |
160237
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Boiling Point |
616.1±55.0 °C at 760 mmHg
|
| Melting Point |
280-281.5℃ (methanol )
|
| Flash Point |
230.8±25.0 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.671
|
| LogP |
2.27
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
24
|
| Complexity |
505
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
IMEYGBIXGJLUIS-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H14O7/c1-22-14-7-13-15(16(21)17(14)23-2)11(20)6-12(24-13)8-3-4-9(18)10(19)5-8/h3-7,18-19,21H,1-2H3
|
| Chemical Name |
2-(3,4-dihydroxyphenyl)-5-hydroxy-6,7-dimethoxychromen-4-one
|
| 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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO : ≥ 25 mg/mL (~75.69 mM)
|
|---|---|
| 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 | 3.0276 mL | 15.1382 mL | 30.2764 mL | |
| 5 mM | 0.6055 mL | 3.0276 mL | 6.0553 mL | |
| 10 mM | 0.3028 mL | 1.5138 mL | 3.0276 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
