Reversible

Pyrrophenone – 1 mg

Brand:
Cayman
CAS:
341973-06-6
Storage:
-20
UN-No:
Non-Hazardous - /

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs).{11920,18018} Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively).{17151} Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency.{18019} Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells,{18019} interleukin-1-induced PGE2 synthesis in mesangial cells,{18019} and the production of PGE2, LTs, and platelet-activating factor by human neutrophils,{17152} always with maximal inhibition at concentrations below 1 μM.  

 

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Description

Reversible, selective inhibitor of cPLA2 with an IC50 value of 4.2 nM in enzyme assays; potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively)

Formal name: N-[[(2S,4R)-1-[2-(2,4-difluorobenzoyl)benzoyl]-4-[(triphenylmethyl)thio]-2-pyrrolidinyl]methyl]-4-[(Z)-(2,4-dioxo-5-thiazolidinylidene)methyl]-benzamide

Synonyms: 

Molecular weight: 850

CAS: 341973-06-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phospholipases||Research Area|Immunology & Inflammation|Innate Immunity

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