525146 sPLA₂-IIA Inhibitor II, KH064 - Calbiochem

525146
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525146-10MG
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      Glass bottle 10 mg
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      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
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      sPLA₂-IIA Inhibitor II, KH064 - Calbiochem Certificates of Analysis

      TitleLot Number
      525146

      References

      Reference overview
      Hansford, 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.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision30-August-2013 JSW
      Synonyms(S)-5-(4-(benzyloxy)phenyl)-4-(7-phenylheptanamido)pentanoic acid, Phospholipase A₂ Group IIA Inhibitor II, PLA2g2a Inhibitor II
      DescriptionA 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.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₃₁H₃₇NO₄
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      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.
      Toxicity Standard Handling
      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.