| Size | Price | Stock | Qty |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Magnolin primarily targets ERK1 and ERK2, which are members of the extracellular signal-regulated kinase family and important signaling molecules in cancer cell metastasis. It inhibits ERK1 and ERK2 with IC50 values of 87 nM and 16.5 nM, respectively. By binding to the active pockets of these kinases, Magnolin inhibits the Ras/ERKs/RSK2 signaling pathway. This inhibition subsequently suppresses NF-kappaB transactivation activity and reduces the production of pro-inflammatory mediators such as tumor necrosis factor-alpha (TNF-alpha) and prostaglandin E2 (PGE2). The compound also blocks the phosphorylation of IkappaBalpha Ser32, which is mediated by ERK1/2/RSK2 signaling, thereby preventing NF-kappaB activation and cell migration.
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| ln Vitro |
Research on seawater, nasal congestion, and anti-inflammatory qualities has been conducted using magnolin, a naturally occurring compound that is concentrated in magnolia flowers. Important signaling molecules in menthol, ERK1 and ERK2, have active pores that are regulated by magnolin. By blocking the extracellular signal regulatory switch (ERK), a crucial signal that controls apoptosis, transformation, and cell migration, magnoli prevents the synthesis of tumor factor-alpha (TNF-alpha) and probene E2 (PGE2). chemical. The administration of Magnolin significantly and dose-dependently inhibited the migration of JB6 Cl41 cells that had been stimulated by EGF treatment. Magnolin prevents NF-κB activation and cell migration by blocking the phosphorylation of IκBα Ser32, which is mediated by ERK1/2/RSK2 signaling [1].
In vitro, Magnolin exhibits potent inhibitory activity against ERK1 and ERK2 with IC50 values of 87 nM and 16.5 nM, respectively. It significantly and dose-dependently inhibits the migration of EGF-stimulated JB6 Cl41 cells. Magnolin also reduces nitric oxide production in LPS-stimulated mouse BV2 microglial cells with an IC50 value of 20,500 nM, as measured by nitrite accumulation using the Griess reagent method. Additionally, it demonstrates inhibitory bioactivity against acetylcholinesterase with an IC50 value of 903 nM and inhibition greater than 90% at concentrations ranging from 0.01 to 100 uM. These properties suggest potential applications in modulating cholinergic neurotransmission and reducing inflammatory responses. |
| ln Vivo |
In vivo, Magnolin has been shown to reduce renal oxidative stress, suppress caspase-3 activity, and increase Bcl-2 expression, demonstrating both anti-inflammatory and antioxidative effects. It ameliorates renal tubular necrosis, apoptosis, and the deterioration of renal function in animal models. The compound's ability to inhibit the Ras/ERKs/RSK2 signaling pathway in vivo contributes to its therapeutic potential in conditions associated with oxidative stress and inflammation. Magnolin has also been studied for its effects on nasal congestion and anti-inflammatory properties, suggesting potential applications in respiratory and inflammatory disorders. Further in vivo studies are needed to fully characterize its efficacy and safety profile.
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| Enzyme Assay |
A typical cell-free assay for Magnolin involves assessing its inhibitory activity against ERK1 and ERK2 kinases. Recombinant ERK1 or ERK2 enzymes are incubated with a peptide substrate, ATP, and various concentrations of Magnolin in a kinase buffer at 30degC for 30-60 minutes. The amount of phosphorylated substrate is measured using a kinase activity assay kit, such as a luminescent ATP detection assay or a radioactive filter-binding assay. The IC50 values are determined by plotting the percentage of kinase activity remaining against the compound concentration. For acetylcholinesterase inhibition, the enzyme is incubated with acetylthiocholine iodide and Magnolin, and the activity is measured using Ellman's method.
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| Cell Assay |
For in vitro cellular experiments, cells such as JB6 Cl41 mouse epidermal cells or BV2 mouse microglial cells are cultured in appropriate media and treated with Magnolin at various concentrations (typically 0.1-100 uM). For migration assays, cells are stimulated with EGF and the inhibitory effect of Magnolin on cell migration is assessed using wound healing or Boyden chamber assays. For anti-inflammatory studies, BV2 cells are stimulated with LPS and Magnolin is added simultaneously. After 20 hours of incubation, nitrite accumulation in the culture medium is measured using the Griess reagent to assess nitric oxide production. Cell viability is typically assessed using MTT or CCK-8 assays to ensure that observed effects are not due to cytotoxicity.
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| Animal Protocol |
In vivo animal experiments with Magnolin typically involve oral administration in rodent models. A common protocol involves administering Magnolin to mice or rats at doses ranging from 10-50 mg/kg body weight, either as a single dose or daily for 1-4 weeks. For renal protection studies, animals are subjected to renal ischemia-reperfusion injury or treated with nephrotoxic agents, and Magnolin is administered prophylactically or therapeutically. Kidney function is assessed by measuring serum creatinine and blood urea nitrogen levels, and renal tissue is collected for histopathological examination and analysis of oxidative stress markers, caspase-3 activity, and Bcl-2 expression. Blood and tissue samples are collected for pharmacokinetic and biochemical analysis.
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| ADME/Pharmacokinetics |
Magnolin is a small molecule with a molecular weight of 416.46 g/mol and a molecular formula of C23H28O7. It is soluble in DMSO (250 mg/mL) and has a density of 1.178 g/cm3. As a natural product, its pharmacokinetic properties are not extensively characterized, but it is expected to have moderate oral bioavailability due to its lipophilic nature (LogP 2.78). The compound is stable as a powder at -20degC for up to 3 years and in solution at -80degC for 1 year. Further pharmacokinetic studies, including absorption, distribution, metabolism, and excretion profiles, are needed to fully characterize its properties for therapeutic development.
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| Toxicity/Toxicokinetics |
The toxicity profile of Magnolin has not been extensively characterized in preclinical studies. However, as a major component of Magnolia liliiflora, which has been used in traditional medicine, it is generally considered to have a favorable safety profile at pharmacological doses. In vitro studies have shown that Magnolin exhibits inhibitory activity against acetylcholinesterase, which may have implications for cholinergic signaling at higher concentrations. The compound should be handled with standard laboratory precautions, and its use is intended for research purposes only. Further toxicological studies are needed to establish its full safety profile for potential therapeutic applications.
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| References | |
| Additional Infomation |
Magnolin has been reported in Geranium platyanthum, Annona mucosa, and other organisms with relevant data. See also: Flower apex (partial) of Centipeda minima.
Magnolin is a naturally occurring lignan and the major bioactive component of Magnolia liliiflora (Xin-yi). It targets ERK1 and ERK2 with IC50 values of 87 nM and 16.5 nM, respectively, thereby inhibiting the Ras/ERKs/RSK2 signaling pathway. The compound has demonstrated anti-inflammatory and antioxidative effects both in vitro and in vivo, reducing renal oxidative stress, suppressing caspase-3 activity, and increasing Bcl-2 expression. Magnolin also inhibits nitric oxide production in LPS-stimulated microglial cells and exhibits acetylcholinesterase inhibitory activity. It has been studied for its potential applications in renal protection, inflammation, and cancer research. Magnolin is available as a research compound and is not approved for clinical use. |
| Molecular Formula |
C23H28O7
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|---|---|
| Molecular Weight |
416.46422
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| Exact Mass |
416.183
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| CAS # |
31008-18-1
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| PubChem CID |
169234
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
536.9±50.0 °C at 760 mmHg
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| Flash Point |
215.6±30.0 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.542
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| LogP |
2.78
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
532
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| Defined Atom Stereocenter Count |
4
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| SMILES |
COC1=C(C=C(C=C1)[C@@H]2[C@H]3CO[C@@H]([C@H]3CO2)C4=CC(=C(C(=C4)OC)OC)OC)OC
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| InChi Key |
MFIHSKBTNZNJIK-RZTYQLBFSA-N
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| InChi Code |
InChI=1S/C23H28O7/c1-24-17-7-6-13(8-18(17)25-2)21-15-11-30-22(16(15)12-29-21)14-9-19(26-3)23(28-5)20(10-14)27-4/h6-10,15-16,21-22H,11-12H2,1-5H3/t15-,16-,21+,22+/m0/s1
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| Chemical Name |
(3S,3aR,6S,6aR)-3-(3,4-dimethoxyphenyl)-6-(3,4,5-trimethoxyphenyl)-1,3,3a,4,6,6a-hexahydrofuro[3,4-c]furan
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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 (~240.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4012 mL | 12.0060 mL | 24.0119 mL | |
| 5 mM | 0.4802 mL | 2.4012 mL | 4.8024 mL | |
| 10 mM | 0.2401 mL | 1.2006 mL | 2.4012 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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