Mofezolac (Synonyms: N-22) |
| رقم الكتالوجGC61843 |
Mofezolac ، عقار مضاد للالتهابات غير ستيرويدي (NSAID) ، هو مثبط انتقائي ، قابل للانعكاس ونشط عن طريق الفم مع مثبطات COX-1 مع IC50 من 1.44 نانومتر
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Cas No.: 78967-07-4
Sample solution is provided at 25 µL, 10mM.
Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities[1].
Mofezolac inhibits platelet aggregation with an IC50 of 0.45 µM in human platelet rich plasma (hPRP) assay[2]. Mofezolac slightly increase Bortezomib cytotoxic effect on multiple myeloma (MM) cell lines (NCI-H929 and RPMI-8226) and affects MM cell cycle and apoptosis when co-administered with the proteasome inhibitor Bortezomib[2].
Mofezolac (1-30 mg/kg; oral administration; once) treatment results in the suppression of writhing induced by the intraperitoneal injection of phenyl-p-benzoquinone in mice[1].
References:
[1]. K Goto, et al. Analgesic effect of mofezolac, a non-steroidal anti-inflammatory drug, against phenylquinone-induced acute pain in mice. Prostaglandins Other Lipid Mediat. 1998 Jul;56(4):245-54.
[2]. Maria Laura Pati, et al. Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability. Eur J Med Chem. 2019 Feb 15;164:59-76.
| Cas No. | 78967-07-4 | SDF | |
| المرادفات | N-22 | ||
| Canonical SMILES | O=C(O)CC1=C(C2=CC=C(OC)C=C2)C(C3=CC=C(OC)C=C3)=NO1 | ||
| Formula | C19H17NO5 | M.Wt | 339.34 |
| الذوبان | DMSO : 100 mg/mL (294.69 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9469 mL | 14.7345 mL | 29.469 mL |
| 5 mM | 589.4 μL | 2.9469 mL | 5.8938 mL |
| 10 mM | 294.7 μL | 1.4734 mL | 2.9469 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.50%
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Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)
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