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| Replacement Information |
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| Empirical Formula |
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| C₄₉H₄₄F₂N₄O₅S |
| Description | |
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| Overview | This product has been discontinued. A cell-permeable 1,2,4-trisubstituted pyrrolidine derivative that acts as a highly specific and potent inhibitor of cPLA2α (cytosolic phospholipase A2α) (IC50 = 1.8 nM). Blocks the release of eicosanoids from A23187-stimulated THP-1 cells (IC50 = 22 nM for arachidonic acid, 31 nM for prostaglandin E2, 13 nM for leukotriene C4). Displays over 230-fold greater potency in the enzyme assay and ~ 3900-fold greater potency in the cellular assay than AACOCF3 (Cat. No. 100109). Does not exert any significant effects on the activities of cycloxygenase and 5-lipoxygenase. |
| Catalogue Number | 525143 |
| Brand Family | Calbiochem® |
| Synonyms | N-{(2S,4R)-4-(Biphenyl-2-ylmethyl-isobutyl-amino)-1-[2-(2,4-difluorobenzoyl)-benzoyl]-pyrrolidin-2-ylmethyl}-3-[4-(2,4-dioxothiazolidin-5-ylidenemethyl)-phenyl]acrylamide, HCl, cPLA2α Inhibitor |
| References | |
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| References | Seno, K., et al. 2000. J. Med. Chem. 43, 1041. |
| Product Information | |
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| ATP Competitive | N |
| Form | Off-white solid |
| Hill Formula | C₄₉H₄₄F₂N₄O₅S |
| Chemical formula | C₄₉H₄₄F₂N₄O₅S |
| Hygroscopic | Hygroscopic |
| Reversible | N |
| Structure formula Image | |
| Applications | |
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| Application | cPLA2α Inhibitor is a cell-permeable, highly specific and potent inhibitor of cPLA2α (cytosolic phospholipase A2α) (IC50 = 1.8 nM). |
| Biological Information | |
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| Primary Target | cPLA2α |
| Primary Target IC<sub>50</sub> | 1.8 nM against cPLA2α (cytosolic phospholipase A2α |
| Purity | ≥98% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
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| Safety Information according to GHS |
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| Product Usage Statements |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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