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Cyclosporin H

现货
Catalog No.
B5921
甲酰肽受体拮抗剂
组合的产品项目
规格价格库存 数量
25mg
¥ 9,000.00
Ship with 10-15 days
5mg
¥ 3,000.00
Ship with 10-15 days

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Background

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].

References:
[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.

Chemical Properties

Physical AppearanceA white powder
StorageStore at -20°C
M.Wt1202.61
Cas No.83602-39-5
FormulaC62H111N11O12
SolubilitySoluble in DMSO
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
SDFDownload SDF
Canonical SMILESC/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
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

Cyclosporin H