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525146 sPLA₂-IIA Inhibitor II, KH064 - Calbiochem

sPLA₂-IIA Inhibitor II, KH064 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (S)-5-(4-(benzyloxy)phenyl)-4-(7-phenylheptanamido)pentanoic acid, Phospholipase A₂ Group IIA Inhibitor II, PLA2g2a Inhibitor II

525146
  
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Přehled

Replacement Information
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
Global Trade Item Number
Katalogové číslo GTIN
525146 0

Documentation

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

TitleLot Number
525146

References

Přehled odkazů
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 Protect from light
+2°C to +8°C
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.