Dimethylfraxetin
Based on 1 Customer Validation
Dimethylfraxetin is a Carbonic anhydrase inhibitor, with a Ki value of 0.0097 μM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.81%
- CAS No.: 6035-49-0
- Formule: C12H12O5
- Masse moléculaire:236.22
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Ki: 0.0097 μM (Carbonic anhydrase)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Neutrophil | IC50 |
>30 μM
Compound: 7
|
Antiinflammatory activity in human neutrophils assessed as inhibition of fMet-Leu-Phe/Cytochalasin B-induced superoxide anion generation treated 5 mins before fMet-Leu-Phe/Cytochalasin B challenge by spectrophotometry
Antiinflammatory activity in human neutrophils assessed as inhibition of fMet-Leu-Phe/Cytochalasin B-induced superoxide anion generation treated 5 mins before fMet-Leu-Phe/Cytochalasin B challenge by spectrophotometry
|
[PMID: 19203247] |
| Neutrophil | IC50 |
>30 μM
Compound: 7
|
Antiinflammatory activity in human neutrophils assessed as inhibition of fMet-Leu-Phe/Cytochalasin B-induced elastase release treated 5 mins before fMet-Leu-Phe/Cytochalasin B challenge
Antiinflammatory activity in human neutrophils assessed as inhibition of fMet-Leu-Phe/Cytochalasin B-induced elastase release treated 5 mins before fMet-Leu-Phe/Cytochalasin B challenge
|
[PMID: 19203247] |
| Neutrophil | IC50 |
>50 μM
Compound: 12
|
Antiinflammatory activity in human neutrophils assessed as inhibition of formyl-L-methionyl-L-leucyl-L-phenylalanine/cytochalasin B-induced elastase release
Antiinflammatory activity in human neutrophils assessed as inhibition of formyl-L-methionyl-L-leucyl-L-phenylalanine/cytochalasin B-induced elastase release
|
[PMID: 18211005] |
| Neutrophil | IC50 |
>50 μM
Compound: 6,7,8-trimethoxycoumarin
|
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/Cytochalasin B-induced elastase release
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/Cytochalasin B-induced elastase release
|
[PMID: 18817445] |
| Neutrophil | IC50 |
47.1 μM
Compound: 15
|
Antiinflammatory activity in human neutrophils assessed as fMLP-induced superoxide release after 5 mins by spectrometry
Antiinflammatory activity in human neutrophils assessed as fMLP-induced superoxide release after 5 mins by spectrometry
|
[PMID: 17822293] |
| Neutrophil | IC50 |
48.6 μM
Compound: 6,7,8-trimethoxycoumarin
|
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced superoxide radical anion generation
Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/cytochalasin B-induced superoxide radical anion generation
|
[PMID: 18817445] |
| Neutrophil | IC50 |
49.52 μM
Compound: 12
|
Antiinflammatory activity in human neutrophils assessed as inhibition of formyl-L-methionyl-L-leucyl-L-phenylalanine/cytochalasin B-induced superoxide anion generation
Antiinflammatory activity in human neutrophils assessed as inhibition of formyl-L-methionyl-L-leucyl-L-phenylalanine/cytochalasin B-induced superoxide anion generation
|
[PMID: 18211005] |
At CA I there is one stand out compound being Dimethylfraxetin (compound 17), a nanomolar CA I inhibitor. This trimethoxy coumarin is the most potent of any of the NP coumarins across the six CA isozymes of the present study[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 6035-49-0
-
Appearance Solid
-
Masse moléculaire 236.22
-
Formule C12H12O5
-
Color White to yellow
-
SMILES
O=C1C=CC2=CC(OC)=C(OC)C(OC)=C2O1
-
Synonyms
6,7,8-Trimethoxycoumarin; Fraxetin dimethyl ether
-
Structure Classification
-
Initial Source
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (529.17 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. 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. 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)
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: ≥ 2.08 mg/mL (8.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (8.81 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
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.
Protocole
Inhibitor (including Dimethylfraxetin) and enzyme solutions are preincubated together for 6 h at room temperature prior to assay, in order to allow for the formation of the enzyme-inhibitor complex[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
-
Fiche technique (275 KB)
-
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
-
Instruction de manipulation (2659 KB)
Références
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. 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 | 4.2333 mL | 21.1667 mL | 42.3334 mL | 105.8335 mL |
| 5 mM | 0.8467 mL | 4.2333 mL | 8.4667 mL | 21.1667 mL | |
| 10 mM | 0.4233 mL | 2.1167 mL | 4.2333 mL | 10.5834 mL | |
| 15 mM | 0.2822 mL | 1.4111 mL | 2.8222 mL | 7.0556 mL | |
| 20 mM | 0.2117 mL | 1.0583 mL | 2.1167 mL | 5.2917 mL | |
| 25 mM | 0.1693 mL | 0.8467 mL | 1.6933 mL | 4.2333 mL | |
| 30 mM | 0.1411 mL | 0.7056 mL | 1.4111 mL | 3.5278 mL | |
| 40 mM | 0.1058 mL | 0.5292 mL | 1.0583 mL | 2.6458 mL | |
| 50 mM | 0.0847 mL | 0.4233 mL | 0.8467 mL | 2.1167 mL | |
| 60 mM | 0.0706 mL | 0.3528 mL | 0.7056 mL | 1.7639 mL | |
| 80 mM | 0.0529 mL | 0.2646 mL | 0.5292 mL | 1.3229 mL | |
| 100 mM | 0.0423 mL | 0.2117 mL | 0.4233 mL | 1.0583 mL |