504924 Sigma-AldrichIndomethacin, 2ʹ-Trifluoromethyl - Calbiochem
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Overview
Key Spec Table
| Empirical Formula |
|---|
| C₁₉H₁₃ClF₃NO₄ |
| Description | |
|---|---|
| Overview | This product has been discontinued. A cell-permeable, bioavailable 2′-trifluoromethyl analog of Indomethacin (Cat. No. 405268) that acts as a highly potent, time-dependent inhibitor of cyclooxygenase -2 (COX-2; IC50 = 267 and 388 nM for mouse and human COX-2, respectively) and its several mutant forms. Does not affect COX-1 activity even at high concentrations (IC50 >100 µM). Interacts with human COX-2 with much greater affinity than indomethacin (KI = 1.5 vs 13 µM) and blocks COX-2 dependent arachidonic acid oxygenation (IC50 = 150 nM in 1483 human head and neck squamous cell carcinoma cells). Further, minimizes swelling in carrageenan-induced rat paw edema model (EC50 = 1.7 mg/kg, p.o.) with no gastrointestinal bleeding at higher doses (10 mg/kg). |
| Catalogue Number | 504924 |
| Brand Family | Calbiochem® |
| Synonyms | Indomethacin, 2ʹ-Trifluoromethyl; Indomethacin, 2-CF₃, CF₃-Indomethacin; CF₃-INDO |
| References | |
|---|---|
| References | Blobaum, A.L., et al. 2013. ACS Med. Chem. Lett. 4, 486. |
| Product Information | |
|---|---|
| Form | White powder |
| Hill Formula | C₁₉H₁₃ClF₃NO₄ |
| Chemical formula | C₁₉H₁₃ClF₃NO₄ |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Primary Target | COX-2 |
| Primary Target IC<sub>50</sub> | 267 and 388 nM for mouse and human COX-2, respectively |
| Purity | ≥98% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 504924 | 0 |