Methylhydroquinone
Based on 1 Customer Validation
Methylhydroquinone is an orally active COX inhibitor with IC50s of 480.7 μM and 52.2 μM for ovine COX-1 and human recombinant COX-2, respectively. Methylhydroquinone has potential DNA damaging effects: 1) inhibiting COX-1 to reduce prostaglandin synthesis and exert anti-inflammatory activity; 2) inducing DNA single-strand breaks. Methylhydroquinone exerts its effects by competitively binding to the active sites of COX-1 (such as Tyr385, Met522) and non-covalent interactions.
For research use only. We do not sell to patients.
- Purity : 99.91%
- CAS No.: 95-71-6
- Formula: C7H8O2
- Molecular Weight:124.14
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
5.7 μM
Compound: 22
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Growth inhibition of human A2780 cells after 72 hrs by SRB assay
Growth inhibition of human A2780 cells after 72 hrs by SRB assay
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[PMID: 29519737] |
| A2780cis | IC50 |
4.7 μM
Compound: 22
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Growth inhibition of human A2780cis cells after 72 hrs by SRB assay
Growth inhibition of human A2780cis cells after 72 hrs by SRB assay
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[PMID: 29519737] |
| OVCAR-8 | IC50 |
6.2 μM
Compound: 22
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Growth inhibition of human OVCAR8 cells after 72 hrs by SRB assay
Growth inhibition of human OVCAR8 cells after 72 hrs by SRB assay
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[PMID: 29519737] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Gastric Pyloric Mucosa Injury Model in Male F344 rats (7 weeks old, 25-30 g)
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Dosage:200 mg/kg (aqueous solution)
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Administration:Single gastric intubation (2 h prior to sacrifice)
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Result:Significantly increased DNA single-strand breaks) in the pyloric mucosa 2 h post-administration, but did not induce detectable unscheduled DNA synthesis (UDS).
Weakly promoted tumorigenesis by increasing ornithine decarboxylase (ODC) activity (6-fold) and replicative DNA synthesis (RDS) at 24 h and 16 h, respectively.
Chemical Information
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CAS No. 95-71-6
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Appearance Solid
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Molecular Weight 124.14
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Formula C7H8O2
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Color White to off-white
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SMILES
CC1=CC(O)=CC=C1O
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Structure Classification
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Initial Source
Burkholderia sp. NF100.
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
In Vitro:
DMSO : ≥ 100 mg/mL (805.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (40.28 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (40.28 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Cotton Pellet Granuloma
Cotton pellet granuloma is a classical in vivo chronic inflammation model used to evaluate the anti-inflammatory potential of test substances by measuring their ability to inhibit granuloma tissue formation around an implanted foreign body (cotton pellet) in rodents. The method is based on the biological response to a sterile implanted material, which induces proliferative phase inflammation characterized by fibroblast proliferation and collagen-rich granuloma formation, and the final readout reflects the extent of chronic inflammatory tissue growth surrounding the pellet. In multiple preclinical pharmacological evaluations, inhibition of cotton pellet-induced granuloma formation has been used as an indicator of anti-inflammatory activity in both synthetic and natural product screening contexts.
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (273 KB)
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SDS (950 KB)
- English - EN (950 KB)
- Français - FR (950 KB)
- Deutsch - DE (950 KB)
- Norwegian - NO (950 KB)
- Español - ES (950 KB)
- Swedish - SV (950 KB)
- Italian - IT (950 KB)
- Korean - KR (950 KB)
- Portuguese - PT (950 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 8.0554 mL | 40.2771 mL | 80.5542 mL | 201.3855 mL |
| 5 mM | 1.6111 mL | 8.0554 mL | 16.1108 mL | 40.2771 mL | |
| 10 mM | 0.8055 mL | 4.0277 mL | 8.0554 mL | 20.1386 mL | |
| 15 mM | 0.5370 mL | 2.6851 mL | 5.3703 mL | 13.4257 mL | |
| 20 mM | 0.4028 mL | 2.0139 mL | 4.0277 mL | 10.0693 mL | |
| 25 mM | 0.3222 mL | 1.6111 mL | 3.2222 mL | 8.0554 mL | |
| 30 mM | 0.2685 mL | 1.3426 mL | 2.6851 mL | 6.7129 mL | |
| 40 mM | 0.2014 mL | 1.0069 mL | 2.0139 mL | 5.0346 mL | |
| 50 mM | 0.1611 mL | 0.8055 mL | 1.6111 mL | 4.0277 mL | |
| 60 mM | 0.1343 mL | 0.6713 mL | 1.3426 mL | 3.3564 mL | |
| 80 mM | 0.1007 mL | 0.5035 mL | 1.0069 mL | 2.5173 mL | |
| 100 mM | 0.0806 mL | 0.4028 mL | 0.8055 mL | 2.0139 mL |