Cyclosporin H

mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail

Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.

Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody

Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay

SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.

Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
Physical Appearance | A white powder |
Storage | Store at -20°C |
M.Wt | 1202.61 |
Cas No. | 83602-39-5 |
Formula | C62H111N11O12 |
Solubility | Soluble 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 |
SDF | Download SDF |
Canonical SMILES | C/C([H])=C([H])/C[[email protected]@]([[email protected]](O)([H])[[email protected]@](N1C)([H])/C(O)=N\[[email protected]@](C(N(CC(N([[email protected]@](/C(O)=N/[[email protected]@](C(N([[email protected]@](/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]](C(N([[email protected]@](C(N([[email protected]@](C(N([[email protected]](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 |
Shipping Condition | Ship with blue ice, or upon other requests. |
General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
- View current batch:
Chemical structure
