| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 2mg | |||
| Other Sizes |
| Targets |
c-Met/HGFR; FabI (enoyl-ACP reductase).
|
|---|---|
| ln Vitro |
Human breast cancer cell lines MDA-MB-231, MDA-468, BT-474, SK BR-3, MCF7, and MCF7-dox cannot proliferate when meleagrin is present [3]. Breast cancer cell lines' HGF-induced cell migration and invasion are inhibited by meleagrin in a dose-dependent manner [3].
Meleagrin is a class of FabI inhibitor. It serves as a lead c-Met inhibitory entity for controlling c-Met-dependent metastatic and invasive breast malignancies. The compound has antimicrobial, antiviral, and antiproliferative activities. It has been shown to have antitumor activities. |
| ln Vivo |
In an orthotopic athymic nude mouse model, meleagrin efficiently suppresses the growth of invasive triple-negative breast carcinoma cells [3].
Meleagrin has demonstrated in vivo antitumor activities in preclinical studies. It has been studied for its antifouling properties in barnacle models. The compound has also been investigated for its role in the biosynthesis of mycotoxins in Penicillium species. Further in vivo studies would be needed to fully characterize its therapeutic potential in cancer. |
| Enzyme Assay |
In vitro enzyme assays for FabI inhibition use recombinant FabI enzyme and the substrate crotonyl-CoA. Meleagrin is incubated with FabI, NADH, and crotonyl-CoA at varying concentrations (typically 0.01-100 µM). Enzyme activity is measured spectrophotometrically at 340 nm by monitoring NADH oxidation. IC50 values are calculated from dose-response curves. For c-Met inhibition, kinase assays using recombinant c-Met and appropriate peptide substrates are performed.
|
| Cell Assay |
In vitro cellular assays are performed using breast cancer cell lines (e.g., MDA-MB-231 or MCF-7) or other cancer cell lines. Cells are treated with Meleagrin at concentrations ranging from 0.01-100 µM for 24-72 hours. Cell proliferation is measured using MTT or CellTiter-Glo assays. c-Met phosphorylation is assessed by Western blot. Apoptosis is measured by Annexin V/PI staining and caspase-3/7 activity. Cell migration and invasion are assessed using Transwell assays. Antimicrobial activity is tested against bacterial cultures.
|
| Animal Protocol |
In vivo efficacy is evaluated in mouse xenograft models using breast cancer cell lines. Meleagrin is administered orally or intraperitoneally at doses ranging from 1-50 mg/kg. Tumor volume is measured by caliper twice weekly. c-Met phosphorylation and downstream signaling markers are assessed in tumor tissues. Body weight and clinical signs are monitored for tolerability. For antifouling studies, barnacle settlement assays are performed.
|
| ADME/Pharmacokinetics |
Meleagrin has a molecular weight of 433.46-433.50 g/mol and molecular formula C23H23N5O4. CAS number: 71751-77-4. Purity ≥98%. Store as a powder at -20°C. Soluble in DMSO. The compound is a natural product isolated from Penicillium fungi. For in vivo use, formulate in suitable vehicle.
|
| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for Meleagrin. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments would include cytotoxicity profiling in mammalian cell lines, hERG channel inhibition for cardiac safety, and CYP450 enzyme inhibition for drug-drug interaction potential. The compound is for research use only.
|
| References |
|
| Additional Infomation |
Meleagrin has been reported to be detected in both Penicillium meleagrinum and Penicillium chrysogenum, and relevant data are available. See also: Meleagrin (note moved to).
Meleagrin is a research-grade natural alkaloid with antimicrobial and anticancer activities. It is not approved for clinical use. The compound belongs to the roquefortine/meleagrin alkaloid family. It is produced by Penicillium chrysogenum and other fungi. Meleagrin is supplied as a powder with high purity and should be stored desiccated at -20°C. It is a valuable tool for studying c-Met signaling and bacterial fatty acid synthesis. |
| Molecular Formula |
C23H23N5O4
|
|---|---|
| Molecular Weight |
433.4598
|
| Exact Mass |
433.175
|
| CAS # |
71751-77-4
|
| PubChem CID |
23728435
|
| Appearance |
Off-white to light yellow solid powder
|
| Density |
1.47g/cm3
|
| Index of Refraction |
1.717
|
| LogP |
2.681
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
32
|
| Complexity |
929
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC(C)(C=C)[C@@]12C=C(C(=O)N\3[C@]1(NC(=O)/C3=C\C4=CN=CN4)N(C5=CC=CC=C25)OC)O
|
| InChi Key |
JTJJJLSLKZFEPJ-ZAYCRUKZSA-N
|
| InChi Code |
InChI=1S/C23H23N5O4/c1-5-21(2,3)22-11-18(29)20(31)27-17(10-14-12-24-13-25-14)19(30)26-23(22,27)28(32-4)16-9-7-6-8-15(16)22/h5-13,29H,1H2,2-4H3,(H,24,25)(H,26,30)/b17-10+/t22-,23-/m0/s1
|
| Chemical Name |
(1S,9R,14E)-11-hydroxy-14-(1H-imidazol-5-ylmethylidene)-2-methoxy-9-(2-methylbut-3-en-2-yl)-2,13,16-triazatetracyclo[7.7.0.01,13.03,8]hexadeca-3,5,7,10-tetraene-12,15-dione
|
| 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: 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.3070 mL | 11.5351 mL | 23.0702 mL | |
| 5 mM | 0.4614 mL | 2.3070 mL | 4.6140 mL | |
| 10 mM | 0.2307 mL | 1.1535 mL | 2.3070 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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