sPLA2 inhibitor

• CAT Number: R026160
• CAS Number: 393569-31-8
• Molecular Formula: C31H37NO4
• Molecular Weight: 487.6
• Purity: ≥95%
• Synonyms: (γS)-γ-[(1-Oxo-7-phenylheptyl)amino]-4-(phenylmethoxy)-benzenepentanoic Acid; ?(S)-5-(4-Benzyloxyphenyl)-4-((7-phenylheptanoyl)amino)pentanoic Acid; KH 064?
• Target: Phospholipase
• Storage: -20°C
• InChI: InChI=1S/C31H37NO4/c33-30(16-10-2-1-5-11-25-12-6-3-7-13-25)32-28(19-22-31(34)35)23-26-17-20-29(21-18-26)36-24-27-14-8-4-9-15-27/h3-4,6-9,12-15,17-18,20-21,28H,1-2,5,10-11,16,19,22-24H2,(H,32,33)(H,34,35)/t28-/m0/s1
• InChIKey: KWLUIYFCMHKLKY-NDEPHWFRSA-N
• SMILES: O=C(CCCCCCC1=CC=CC=C1)N[C@@H](CCC(O)=O)CC(C=C2)=CC=C2OCC3=CC=CC=C3

KH064 is a orally active inhibitor of sPLA2-IIA.

Reference

1:Discovery of AZD2716: A Novel Secreted Phospholipase A2 (sPLA2) Inhibitor for the Treatment of Coronary Artery Disease. Giordanetto F, Pettersen D, Starke I, Nordberg P, Dahlström M, Knerr L, Selmi N, Rosengren B, Larsson LO, Sandmark J, Castaldo M, Dekker N, Karlsson U, Hurt-Camejo E.ACS Med Chem Lett. 2016 Aug 9;7(10):884-889. eCollection 2016 Oct 13. PMID: 27774123 2:Blockade of human group X secreted phospholipase A2 (GX-sPLA2)-induced airway inflammation and hyperresponsiveness in a mouse asthma model by a selective GX-sPLA2 inhibitor. Henderson WR Jr, Oslund RC, Bollinger JG, Ye X, Tien YT, Xue J, Gelb MH.J Biol Chem. 2011 Aug 12;286(32):28049-55. doi: 10.1074/jbc.M111.235812. Epub 2011 Jun 7. PMID: 21652694 Free PMC Article3:The synergistic inhibition of atherogenesis in apoE-/- mice between pravastatin and the sPLA2 inhibitor varespladib (A-002). Shaposhnik Z, Wang X, Trias J, Fraser H, Lusis AJ.J Lipid Res. 2009 Apr;50(4):623-9. doi: 10.1194/jlr.M800361-JLR200. Epub 2008 Nov 21. PMID: 19029066 Free PMC Article4:Suppression of murine endotoxic shock by sPLA2 inhibitor, indoxam, through group IIA sPLA2-independent mechanisms. Yokota Y, Hanasaki K, Ono T, Nakazato H, Kobayashi T, Arita H.Biochim Biophys Acta. 1999 May 18;1438(2):213-22. PMID: 10320804