| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
Isofraxidin targets multiple signaling pathways. It inhibits ERK1/2 phosphorylation, which is involved in cell proliferation and invasion. It attenuates iNOS and COX-2 expression, reducing inflammation. It also inhibits TLR4/MD-2 complex formation, which is involved in innate immune responses. These multiple targets contribute to its anti-inflammatory, anticancer, and immunomodulatory activities.
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| ln Vitro |
Isotrixetine phosphorylates ERK1/2 in cell lines and cell bottoms in vitro, which reduces the production of MMP-7 at non-toxic doses [1]. Isotrixetine forms the TLR4/NF-κB signaling cascade by competitively inhibiting the development of the TLR4/MD-2 complex. Osteoarthritis (OA) may be treated with isofraxidin [2].
Isofraxidin inhibits MMP-7 expression and human hepatocellular carcinoma cell invasion at non-toxic levels by inhibiting ERK1/2 phosphorylation. It also inhibits the expression of iNOS and COX-2. Its anti-inflammatory and anticancer activities have been demonstrated in various in vitro models. It has antibacterial, antioxidant, analgesic, and anti-inflammatory activities. |
| ln Vivo |
Isofraxidin has potential in the treatment of osteoarthritis. This suggests that the compound has in vivo efficacy in animal models of osteoarthritis, where it may reduce inflammation and protect joint tissues. Its anti-inflammatory and antioxidant activities likely contribute to its therapeutic potential in this condition.
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| Enzyme Assay |
Isofraxidin does not have a standard enzyme/receptor binding assay. Its activity is assessed in cell-based assays that measure its effects on various signaling pathways. For example, its ability to inhibit ERK1/2 phosphorylation is measured by Western blot using phospho-specific antibodies. Its effects on MMP-7, iNOS, and COX-2 expression are measured by qPCR or Western blot.
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| Cell Assay |
In vitro cellular assays for isofraxidin involve treating cancer cells or inflammatory cells with the compound and measuring its effects on signaling pathways and gene expression. Its ability to inhibit cell invasion can be assessed using transwell invasion assays. Its anti-inflammatory effects can be assessed by measuring the production of inflammatory mediators.
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| Animal Protocol |
In vivo animal experiments for isofraxidin would involve administering the compound to animal models of cancer, inflammation, or osteoarthritis. Its efficacy in reducing tumor growth, inflammation, or joint damage would be assessed. However, specific in vivo data is not provided in the sources, although its potential in osteoarthritis suggests such studies have been conducted.
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| ADME/Pharmacokinetics |
Isofraxidin has a molecular weight of 222.19 and a molecular formula of C11H10O5. It is a small coumarin compound that is soluble in organic solvents. Its pharmacokinetic properties, such as oral bioavailability and half-life, are not specified in the provided sources. The compound is typically used as an analytical reference standard.
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| Toxicity/Toxicokinetics |
Toxicological data for isofraxidin is not detailed in the provided sources. The compound has been shown to inhibit cell invasion at non-toxic levels, suggesting that it has a favorable safety profile. However, as a research compound, it is not intended for human use. Standard safety precautions should be followed when handling.
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| References |
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| Additional Infomation |
Isofraxidin is a hydroxycoumarin. It has been reported to be found in Phyllanthus urinaria, Artemisia capillaris, and other organisms with relevant data.
Isofraxidin is a coumarin component from Acanthopanax senticosus with antibacterial, antioxidant, analgesic, and anti-inflammatory activities. It inhibits MMP-7 expression and hepatocellular carcinoma cell invasion by inhibiting ERK1/2 phosphorylation. It also attenuates iNOS and COX-2 expression and inhibits TLR4/MD-2 complex formation. It has potential in the treatment of osteoarthritis. Isofraxidin is available from various chemical suppliers for research purposes. |
| Molecular Formula |
C11H10O5
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|---|---|
| Molecular Weight |
222.19
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| Exact Mass |
222.052
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| CAS # |
486-21-5
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| PubChem CID |
5318565
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| Appearance |
Yellow to brown solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
452.1±45.0 °C at 760 mmHg
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| Melting Point |
>300 °C(lit.)
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| Flash Point |
183.2±22.2 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.588
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| LogP |
1.31
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
301
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HOEVRHHMDJKUMZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H10O5/c1-14-7-5-6-3-4-8(12)16-10(6)11(15-2)9(7)13/h3-5,13H,1-2H3
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| Chemical Name |
7-hydroxy-6,8-dimethoxychromen-2-one
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| Synonyms |
Phytodolor; Isofraxidin
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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 : ~250 mg/mL (~1125.16 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.36 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 (9.36 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5007 mL | 22.5033 mL | 45.0065 mL | |
| 5 mM | 0.9001 mL | 4.5007 mL | 9.0013 mL | |
| 10 mM | 0.4501 mL | 2.2503 mL | 4.5007 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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