| 产品详情 |
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| Product Name | sPLA2-IIA Inhibitor II, KH064 |
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| Description | Purity ~95% (HPLC). A reversible, potent, and selective sPLA2-IIA/PLA2g2a (phospholipase A2 group IIA) inhibitor (IC50 = 29nM) that displays much reduced potency against sPLA2-V/PLA2g5 (PLA2 group V; IC50 = 2uM) 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 10uM pretreatment), KH064 is orally available in rats and efficacious in various rat disease models in vivo (5mg/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, KH064 also effectively chelates sPLA2-IIA active site Ca2+ in addition to targeting the enzyme's N-terminal lipid substrate binding site. Formula: C31H37NO4 Solubility: DMSO |
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| Size | 10mg |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | sPLA2-IIA Inhibitor II, KH064 ((S)-5-(4-(benzyloxy)phenyl)-4-(7-phenylheptanamido)pentanoic Acid, Phospholipase A2 Group IIA Inhibitor II, PLA2g2a Inhibitor II) |
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| Gene, Accession, CAS # | n/a |
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| Catalog # | 217807 |
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| Order / More Info | sPLA2-IIA Inhibitor II, KH064 from UNITED STATES BIOLOGICAL |
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| Product Specific References | n/a |
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