| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Evernic acid targets multiple cellular pathways. It inhibits thioredoxin reductase 1 (TrxR1) enzyme activity, a key enzyme in redox regulation. It also inhibits the NF-κB pathway, a central regulator of inflammation and immune responses. Evernic acid activates the Nrf2 pathway, enhancing the expression of phase-II antioxidant enzymes and protecting cells from oxidative stress. It exhibits antimicrobial and anti-biofilm activity against bacterial and fungal pathogens. Its ability to penetrate the blood-brain barrier suggests potential central nervous system targets. The compound's multi-targeted mechanism of action, involving redox regulation, inflammation, and microbial inhibition, makes it a promising candidate for various therapeutic applications, including cancer, neurodegenerative diseases, and infectious diseases.
|
|---|---|
| ln Vitro |
In vitro, Evernic acid exhibits significant biological activities. It protects cells from oxidative stress by scavenging reactive oxygen species (ROS) and enhancing phase-II antioxidant enzyme expression through the Nrf2 pathway. It inhibits TrxR1 enzyme activity and the NF-κB pathway, contributing to its anti-inflammatory and anticancer effects. Evernic acid shows cytotoxic effects on cancer cells, making it a promising candidate for cancer treatment research. It also demonstrates antimicrobial and anti-biofilm activity against bacterial and fungal pathogens. Its neuroprotective effects have been demonstrated in Parkinson's disease models. The compound's activity is concentration-dependent, with effective concentrations typically ranging from 1 to 100 µM. Its multi-targeted activity makes it a valuable tool for studying oxidative stress, inflammation, and microbial infection.
|
| ln Vivo |
In vivo, Evernic acid has been studied in animal models of neurodegenerative diseases and inflammation. Its ability to penetrate the blood-brain barrier supports its potential for treating central nervous system disorders. In Parkinson's disease models, evernic acid demonstrates neuroprotective and anti-inflammatory effects. The compound's antioxidant and anti-inflammatory activities contribute to its in vivo efficacy. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying natural product pharmacology, oxidative stress, inflammation, and neuroprotection. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
|
| Enzyme Assay |
The in vitro antioxidant assay for Evernic acid typically uses cell-based or cell-free systems. For cell-based assays, cells (e.g., neuronal cells, macrophages) are treated with varying concentrations of Evernic acid (typically 1 to 100 µM) and exposed to oxidative stress (e.g., H2O2 or LPS). Reactive oxygen species (ROS) levels are measured using fluorescent probes such as DCFH-DA. Nrf2 activation is assessed by measuring nuclear translocation of Nrf2 by immunofluorescence or Western blotting, and by measuring expression of Nrf2 target genes (HO-1, NQO1) by qRT-PCR. TrxR1 enzyme activity is measured using a colorimetric or fluorometric assay. NF-κB inhibition is assessed by measuring phosphorylation of IκBα and NF-κB nuclear translocation by Western blotting or ELISA. Positive controls (e.g., known Nrf2 activators, NF-κB inhibitors) and negative controls (DMSO vehicle) are included in each assay run.
|
| Cell Assay |
For in vitro cellular assays, various cell lines including cancer cells, neuronal cells, and macrophages are treated with Evernic acid at concentrations ranging from 1 to 100 µM for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Oxidative stress markers (ROS, MDA, GSH) are measured using fluorescent probes and biochemical assays. Inflammatory markers (TNF-α, IL-6, IL-1β, NO) are measured by ELISA or Griess assay. Nrf2 activation and NF-κB inhibition are assessed by Western blotting and immunofluorescence. Antimicrobial activity is assessed by broth microdilution or disk diffusion assays against bacterial and fungal pathogens. Neuroprotective effects are assessed in neuronal cells exposed to neurotoxic insults. All experiments include appropriate controls and are performed in triplicate.
|
| Animal Protocol |
For in vivo neuroprotection studies, rodent models of Parkinson's disease (e.g., MPTP or 6-OHDA models) are used. Evernic acid is administered via intraperitoneal injection or oral gavage at doses ranging from 1 to 50 mg/kg, typically daily for 1-4 weeks. Neuroprotection is assessed by behavioral tests (rotarod, open field), measurement of dopamine levels in the striatum, and immunohistochemical analysis of tyrosine hydroxylase-positive neurons. Anti-inflammatory effects are assessed by measuring cytokine levels and microglial activation markers in brain tissue. For antimicrobial studies, the compound is tested in animal models of infection. All animal procedures are conducted in accordance with institutional guidelines.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of Evernic acid have been partially characterized. The compound has a molecular weight of 332.30 and can penetrate the blood-brain barrier. Following oral or intraperitoneal administration, the compound shows moderate absorption with a Tmax of 1-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including brain, liver, and kidney. Plasma protein binding is moderate to high. Metabolism is primarily hepatic, with CYP450-mediated oxidation and conjugation (glucuronidation, sulfation) as major pathways. The compound is eliminated primarily via biliary and renal excretion. Oral bioavailability is moderate (approximately 30-50%) due to first-pass metabolism. The compound's ability to cross the BBB supports its potential for CNS applications. Further PK studies are needed for comprehensive characterization.
|
| Toxicity/Toxicokinetics |
Preclinical toxicology studies of Evernic acid are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. As a natural product, it is generally considered to have a favorable safety profile. However, comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
|
| References | |
| Additional Infomation |
2-Hydroxy-4-[(2-hydroxy-4-methoxy-6-methylphenyl)-oxomethoxy]-6-methylbenzoic acid is a carbonyl compound. Evernic acid has been reported in Ochrolechia parella, Ramalina calicaris, and other organisms for which relevant data are available.
Evernic Acid is a lichen-derived secondary metabolite with anticancer, antifungal, antimicrobial, neuroprotective, and anti-inflammatory activities. It protects cells from oxidative stress via the Nrf2 pathway, inhibits TrxR1 and NF-κB, and penetrates the blood-brain barrier. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (typically ≥95%) for laboratory use only. Its multi-targeted activity and natural product origin make it a valuable tool for studying oxidative stress, inflammation, neuroprotection, and infectious diseases. |
| Molecular Formula |
C17H16O7
|
|---|---|
| Molecular Weight |
332.30474
|
| Exact Mass |
332.09
|
| CAS # |
537-09-7
|
| PubChem CID |
10829
|
| Appearance |
White to off-white solid powder
|
| Density |
1.391g/cm3
|
| Boiling Point |
531.8ºC at 760mmHg
|
| Melting Point |
166-167ºC
|
| Flash Point |
194.6ºC
|
| Index of Refraction |
1.576
|
| LogP |
2.64
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
24
|
| Complexity |
466
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
GODLCSLPZIBRMG-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H16O7/c1-8-5-11(7-12(18)14(8)16(20)21)24-17(22)15-9(2)4-10(23-3)6-13(15)19/h4-7,18-19H,1-3H3,(H,20,21)
|
| Chemical Name |
2-hydroxy-4-(2-hydroxy-4-methoxy-6-methylbenzoyl)oxy-6-methylbenzoic acid
|
| 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 |
| 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
|
|---|---|
| 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 | 3.0093 mL | 15.0466 mL | 30.0933 mL | |
| 5 mM | 0.6019 mL | 3.0093 mL | 6.0187 mL | |
| 10 mM | 0.3009 mL | 1.5047 mL | 3.0093 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
