產品屬性：

Cas No.: 83602-39-5

別名: N/A

化學名: (3R,6S,9S,12R,13Z,15S,16Z,18S,21S,22Z,24S,30S,31E,33S)-30-ethyl-14,17,23,32-tetrahydroxy-33-((1R,2R,E)-1-hydroxy-2-methylhex-4-en-1-yl)-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,1

分子量: 1202.61

溶解度: Chloroform: Slightly Soluble,Methanol: Slightly Soluble

儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping ConditionEvaluation sample solution : ship with blue ice

All other available size: ship with RT , or blue ice upon request

產品描述：

Cyclosporin H is a potent, selective and competitive formyl peptide receptor (FPR) antagonist with IC50 value of 0.7 μM [1].

The formyl peptide receptor (FPR) is a G protein-coupled receptor involved in chemotaxis and mediating immune cell response to infection.

Cyclosporin H (CsH) is a potent and selective FPR antagonist. In human neutrophils, cyclosporin H inhibited FMLP-induced superoxide anion (O2-) formation. CsH inhibited the binding of FMLP (3 nM) to HL-60 membrane with IC50 and Ki values of 0.7 μM and 0.10 μM, respectively. CsH inhibited GTP hydrolysis stimulated by FMLP (100 nM) with IC50 and Ki values of 1.3 μM and 0.79 μM, respectively. CsH also inhibited the increase of [Ca2+Ii, O2- formation and β-glucuronidase release induced by FMLP with IC50 values of 0.23, 0.6 and 2.2 μM, and with Ki values of 0.08, 0.24, and 0.45 μM, respectively [1][2]. In peripheral blood basophils, CsH (8-800 nM) competitively and concentration-dependently inhibited leukotriene C4 and histamine release activated by FMLP [3]. In eosinophils isolated from bronchoalveolar lavage fluid of mice challenged with inhaled allergen, cyclosporin H increased apoptosis in the presence of 10 U/ml interleukin 5 in a concentration-dependent way. Cyclosporin H also increased apoptosis in the presence of 10 U/ml GM-CSF, but to a lesser extent [4].

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