525146 sPLA₂-IIA Inhibitor II, KH064 - Calbiochem

525146
Price could not be retrieved
Minimum Quantity needs to be mulitiple of
Upon Order Completion More Information
You Saved ()
 
Request Pricing
Limited AvailabilityLimited Availability
Stocked 
Discontinued
Limited Quantities Available
Available
    Remaining : Will advise
      Remaining : Will advise
      Will advise
      Contact Customer Service
      Contact Customer Service
      View Pricing & Availability
      Click To Print This Page

      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      525146-10MG
      Retrieving availability...
      Limited AvailabilityLimited Availability
      Stocked 
      Discontinued
      Limited Quantities Available
      Available
        Remaining : Will advise
          Remaining : Will advise
          Will advise
          Contact Customer Service
          Contact Customer Service

          Glass bottle 10 mg
          Retrieving price...
          Price could not be retrieved
          Minimum Quantity needs to be mulitiple of
          Upon Order Completion More Information
          You Saved ()
           
          Request Pricing
          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
          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

          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.