525143
cPLA2α Inhibitor
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
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EMD Millipore
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23 May 2013
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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.
| Product information | |||
|---|---|---|---|
| Form | Off-white solid | ||
| Primary Target | cPLA2α | ||
| Primary Target IC50 | 1.8 nM | ||
| Secondary target | 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). | ||
| Molar mass | 840.0 | ||
| Protect from Light | Yes | ||
| Hygrocopic | Yes | ||
| Packaged under inert gas | Yes | ||
| Cell permeable | Yes | ||
| Purity | ≥98% by HPLC | ||
| Solubility | 75% Aqueous Acetic Acid or DMSO | ||
| Chemical formula | C49H44F2N4O5S | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | -20°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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