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| 10mg |
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| Targets |
Cycloartenyl ferulate targets IFNγ receptor 1 (IFNγR1) with a binding affinity of Kd = 0.5 μM. By binding to IFNγR1, it activates the JAK1/2-STAT1 signaling pathway. This activation enhances natural killer (NK) cell-mediated anticancer immunity. The compound also exhibits antioxidant, anti-inflammatory, antiallergic, and anticancer activities through modulation of various signaling pathways. It helps scavenge free radicals, protect against lipid peroxidation, and modulate inflammatory signaling pathways. Studies suggest it may also support cholesterol regulation and immune function. Its central nervous system suppressant effects have been observed, with properties different from existing major and minor tranquilizers.
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| ln Vitro |
In vitro studies have demonstrated that Cycloartenyl ferulate binds to IFNγR1 with a Kd of 0.5 μM. This binding activates the JAK1/2-STAT1 signaling pathway. The compound exhibits antioxidant activity by scavenging free radicals and protecting against lipid peroxidation. Its anti-inflammatory activity is mediated through modulation of inflammatory signaling pathways. The compound has demonstrated antiallergic and anticancer activities in various in vitro systems. It enhances NK cell-mediated anticancer immunity. Studies have investigated its effects on the central nervous system. These in vitro findings support its potential therapeutic applications in cancer, inflammation, allergy, and cardiovascular diseases.
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| ln Vivo |
In vivo studies of Cycloartenyl ferulate have demonstrated its effects on the central nervous system. It has been shown to have a suppressant effect on the central nervous system, with properties different from existing major and minor tranquilizers. The compound's antioxidant and anti-inflammatory properties contribute to its potential health benefits in cardiovascular and metabolic diseases. It may support cholesterol regulation and immune function. As a component of gamma-oryzanol derived from rice bran, it has been studied for its various biological activities. Further research is needed to fully characterize its in vivo pharmacokinetic and pharmacodynamic properties and to evaluate its therapeutic potential in various disease models.
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| Enzyme Assay |
In vitro receptor binding assays for Cycloartenyl ferulate involve testing its binding affinity to IFNγR1. Binding affinity is measured using surface plasmon resonance, isothermal titration calorimetry, or radioligand binding assays, with a reported Kd of 0.5 μM. Receptor activation is assessed by measuring JAK1/2-STAT1 signaling pathway activation using Western blotting or ELISA. For antioxidant activity, cell-free systems such as DPPH radical scavenging assays, ABTS assays, or ferric reducing antioxidant power (FRAP) assays are used. Anti-inflammatory activity is evaluated by measuring inhibition of pro-inflammatory mediator production in cell-free or cell-based systems. All assays are performed with appropriate controls and standardized protocols to ensure reproducibility of results.
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| Cell Assay |
In vitro cell-based assays for Cycloartenyl ferulate involve culturing NK cells to evaluate its effects on anticancer immunity. NK cells are treated with the compound and cytotoxicity against cancer cells is measured using standard NK cell killing assays. Cytokine production (e.g., IFN-γ, perforin, granzyme B) is quantified by ELISA. For anti-inflammatory studies, immune cells are treated with the compound and stimulated with inflammatory stimuli; pro-inflammatory cytokine production (e.g., TNF-α, IL-6, IL-1β) is measured. For antioxidant studies, cells are treated with the compound and then exposed to oxidative stress inducers; reactive oxygen species levels are measured using fluorescent probes. Cell viability is assessed using MTT or similar assays. All experiments are performed in triplicate with appropriate controls.
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| Animal Protocol |
In vivo animal experiments for Cycloartenyl ferulate utilize rodent models to evaluate its various biological activities. For central nervous system studies, animals are administered the compound and behavioral, neurological, and physiological parameters are assessed. For anticancer studies, tumor-bearing animals are treated with the compound and tumor growth and NK cell activity are monitored. For anti-inflammatory studies, animals with induced inflammation are treated and inflammatory markers are measured. For cardiovascular and metabolic studies, animals on high-fat diets are treated and metabolic parameters are assessed. Parameters assessed include body weight, organ weights, blood biochemistry, and histopathology. Control groups receiving vehicle alone are included for comparison. All procedures must comply with institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Cycloartenyl ferulate reflect its nature as a large triterpene alcohol. It has a molecular weight of 602.89 and the molecular formula C40H58O4. The compound is lipophilic in nature, which may affect its absorption, distribution, and bioavailability. As a component of gamma-oryzanol from rice bran, it is absorbed through the gastrointestinal tract following dietary consumption. The compound is metabolized through standard xenobiotic pathways. Its large size and lipophilic nature suggest it may have limited water solubility but good membrane permeability. Complete pharmacokinetic profiling including half-life, clearance, volume of distribution, and bioavailability would require further systematic studies using appropriate analytical methods such as high-performance liquid chromatography-mass spectrometry.
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| Toxicity/Toxicokinetics |
The toxicity profile of Cycloartenyl ferulate has been evaluated in the context of its natural occurrence in rice bran and its use as a research chemical. The compound is a natural component of gamma-oryzanol, which is consumed as part of the diet. At dietary levels, it is generally recognized as safe. The compound has demonstrated various biological activities including antioxidant, anti-inflammatory, and anticancer activities, suggesting potential therapeutic applications. Its central nervous system suppressant effects indicate potential for neurological effects that should be carefully evaluated. Proper handling procedures including use of personal protective equipment are recommended when working with pure compound. The compound is intended for research purposes only.
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| References |
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| Additional Infomation |
γ-Oryzanol (TN) is a triterpenoid compound. It has been reported to exist in rice (Oryza sativa), cordyceps (Ophiocordyceps sinensis), and other organisms with relevant data.
Cycloartenyl ferulate (CAS# 21238-33-5) is also known as cycloartenol ferulate, cycloartenol ferulic acid ester, and γ-oryzanol derivative. It has the molecular formula C40H58O4 and a molecular weight of 602.89. The compound is a typical triterpene alcohol with various biological activities including anti-oxidative, antiallergic, anti-inflammatory, and anticancer activities. It enhances NK cell-mediated anticancer immunity by binding to IFNγR1 with a Kd of 0.5 μM and activating the JAK1/2-STAT1 signaling pathway. The compound exhibits potent antioxidant and anti-inflammatory properties. It helps scavenge free radicals, protect against lipid peroxidation, and modulate inflammatory signaling pathways. It may support cholesterol regulation and immune function. The compound has a suppressant effect on the central nervous system. |
| Molecular Formula |
C40H58O4
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| Molecular Weight |
602.89
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| Exact Mass |
602.434
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| CAS # |
21238-33-5
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| PubChem CID |
5282164
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| Appearance |
White to off-white solid
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| Density |
1.1g/cm3
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| Boiling Point |
663.2ºC at 760 mmHg
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| Flash Point |
193.8ºC
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| Vapour Pressure |
3.38E-18mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
10.147
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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 |
9
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| Heavy Atom Count |
44
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| Complexity |
1150
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC(CCC=C(C)C)C1CCC2(C1(CCC34C2CCC5C3(C4)CCC(C5(C)C)OC(=O)C=CC6=CC(=C(C=C6)O)OC)C)C
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| InChi Key |
FODTZLFLDFKIQH-FSVGXZBPSA-N
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| InChi Code |
InChI=1S/C40H58O4/c1-26(2)10-9-11-27(3)29-18-20-38(7)33-16-15-32-36(4,5)34(19-21-39(32)25-40(33,39)23-22-37(29,38)6)44-35(42)17-13-28-12-14-30(41)31(24-28)43-8/h10,12-14,17,24,27,29,32-34,41H,9,11,15-16,18-23,25H2,1-8H3/b17-13+/t27-,29-,32+,33+,34+,37-,38+,39-,40+/m1/s1
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| Chemical Name |
[(1S,3R,6S,8R,11S,12S,15R,16R)-7,7,12,16-tetramethyl-15-[(2R)-6-methylhept-5-en-2-yl]-6-pentacyclo[9.7.0.01,3.03,8.012,16]octadecanyl] (E)-3-(4-hydroxy-3-methoxyphenyl)prop-2-enoate
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| Synonyms |
Cycloartenol ferulate; Cycloartenol ferulic acid ester; Cycloartenyl ferulate
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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) |
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 | 1.6587 mL | 8.2934 mL | 16.5868 mL | |
| 5 mM | 0.3317 mL | 1.6587 mL | 3.3174 mL | |
| 10 mM | 0.1659 mL | 0.8293 mL | 1.6587 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05922800
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