Cyclosporin H
(Synonyms: 环孢菌素H) 目录号 : GC15319A formyl peptide receptor antagonist
Cas No.:83602-39-5
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
- Datasheet
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.
Cas No. | 83602-39-5 | SDF | |
别名 | 环孢菌素H | ||
化学名 | (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-1,4,7,10,13,16,19,22,25,28,31-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 | ||
分子式 | C62H111N11O12 | 分子量 | 1202.61 |
溶解度 | Chloroform: Slightly Soluble,Methanol: Slightly Soluble; DMSO: 100 mg/mL (83.15 mM) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 0.8315 mL | 4.1576 mL | 8.3152 mL |
5 mM | 0.1663 mL | 0.8315 mL | 1.663 mL |
10 mM | 0.0832 mL | 0.4158 mL | 0.8315 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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