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Description

A highly hydrophobic cyclic pentapeptide that selectively binds and acts as a potent inhibitor of human type IIA secreted phospholipase A2 (sPLA2-IIA) (IC50 = 12.8 µ,M). Reported to effectively block sPLA2-IIA-induced PGE2 production at 100 nM in human rheumatoid synoviocytes and is non-toxic at doses up to 10 µ,M. Does not have any significant effect on the activities of porcine sPLA2-IB, Naja naja sPLA2-IB, or Crotalus durissus sPLA2-IIA at 10 µ,M., A highly hydrophobic cyclic pentapeptide that selectively binds and acts as a potent inhibitor of sPLA2-IIA (human type IIA secreted phospholipase A2, IC50 = 12.8 muM). Shown to effectively block sPLA2-IIA-induced PGE2 production at 100 nM in human rheumatoid synoviocytes and is non-toxic at doses up to 10 muM. Does not have any significant effect on the activities of porcine sPLA2-IB, Naja naja sPLA2-IB, or Crotalus durissus sPLA2-IIA even at 10 muM concentration.