525146-M

sPLA₂-IIA Inhibitor II, KH064

• 別名: (S)-5-(4-(benzyloxy)phenyl)-4-(7-phenylheptanamido)pentanoic acid, Phospholipase A₂ Group IIA Inhibitor II, PLA2g2a Inhibitor II
• UNSPSCコード: 12352200

特性

• アッセイ: ≥95% (HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 100 mg/mL
• 保管温度: 2-8°C

詳細

詳細

A 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.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

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.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable