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Cyclosporin H Catalog No.GC15319

Selective and competitive formyl peptide receptor antagonist

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 83602-39-5 SDF
Synonyms N/A
Chemical Name (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-1,4,7,10,13,16,19,22,25,28,31-undecaazacycl
Canonical SMILES C/C([H])=C([H])/C[C@@]([C@](O)([H])[C@@](N1C)([H])/C(O)=N\[C@@](C(N(CC(N([C@@](/C(O)=N/[C@@](C(N([C@@](/C(O)=N/[C@@](/C(O)=N/[C@](C(N([C@@](C(N([C@@](C(N([C@](C1=O)([H])C(C)C)C)=O)([H])CC(C)C)C)=O)([H])CC(C)C)C)=O)([H])C)([H])C)([H])CC(C)C)C)=O)([H])C(C)C
Formula C62H111N11O12 M.Wt 1202.61
Solubility Chloroform: Slightly Soluble,Methanol: Slightly Soluble Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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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].

[1].  Wenzel-Seifert K, Seifert R. Cyclosporin H is a potent and selective formyl peptide receptor antagonist. Comparison with N-t-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L- leucyl-L-phenylalanine and cyclosporins A, B, C, D, and E. J Immunol, 1993, 150(10): 4591-4599.
[2].  Wenzel-Seifert K, Grünbaum L, Seifert R. Differential inhibition of human neutrophil activation by cyclosporins A, D, and H. Cyclosporin H is a potent and effective inhibitor of formyl peptide-induced superoxide formation. J Immunol, 1991, 147(6): 1940-1946.
[3].  de Paulis A, Ciccarelli A, de Crescenzo G, et al. Cyclosporin H is a potent and selective competitive antagonist of human basophil activation by N-formyl-methionyl-leucyl-phenylalanine. J Allergy Clin Immunol, 1996, 98(1): 152-164.
[4].  Kitagaki K, Nagai H, Hayashi S, et al. Facilitation of apoptosis by cyclosporins A and H, but not FK506 in mouse bronchial eosinophils. Eur J Pharmacol, 1997, 337(2-3): 283-289.