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525146 sPLA₂-IIA Inhibitor II, KH064 - Calbiochem

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525146
  
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      Übersicht

      Description
      OverviewA reversible, potent, and selective sPLA2-IIA/PLA2g2a (phospholipase A2 group IIA) inhibitor (IC50 = 29 nM) that displays much reduced potency against sPLA2-V/PLA2g5 (PLA2 group V; IC50 = 2 µM) and is reported not to affect the activity of cytosolic cPLA2, Ca2+-independent iPLA2, 30 human GPCRs, and 25 other enzymes. In addition to being useful in studying PLA2g2a-mediated cellular responses in cultures in vitro (100% inhibition of LPS-induced PGE2 production in HMC-1 cells; 15 min 10 µM pretreatment), KH064 is orally available in rats and efficacious in various rat disease models in vivo (5 mg/kg p.o.), including adjuvant-induced arthritis, spontaneous hypertension, high fat diet-induced metabolic disorders. Comparing to the substrate-competitive inhibitor c(2NapA)LS(2NapA)R (Cat. No. 525145), KH064 also effectively chelates sPLA2-IIA active site Ca2+ in addition to targeting the enzyme's N-terminal lipid substrate binding site.
      Catalogue Number525146
      Brand Family Calbiochem®
      Synonyms(S)-5-(4-(benzyloxy)phenyl)-4-(7-phenylheptanamido)pentanoic acid, Phospholipase A₂ Group IIA Inhibitor II, PLA2g2a Inhibitor II
      References
      ReferencesHansford, K. A., et al. 2003. Chembiochem. 4, 181.
      Iyer, A., et al. 2012. Diabetes. 61, 2320,
      Levick, S., et al. 2006. J Immunol. 176, 7000.
      Product Information
      FormWhite solid
      Hill FormulaC₃₁H₃₇NO₄
      Chemical formulaC₃₁H₃₇NO₄
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Purity≥95% by HPLC
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Bestellnummer GTIN
      525146 0