Cyclosporin H (Synonyms: 5-(N-methyl-D-valine)-Cyclosporin A, Sandoz 37-839) |
| Katalog-Nr.GC15319 |
Cyclosporin H ist ein selektiver und wirksamer Inhibitor von FPR-1 (Formylpeptidrezeptor 1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 83602-39-5
Sample solution is provided at 25 µL, 10mM.
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Cyclosporin H is a potent and selective formyl peptide receptor (FPR) antagonist with an IC50 value of 0.7μM[1]. Cyclosporin H can be used as a viral transduction enhancer to improve the efficiency of lentiviral transduction in hematopoietic stem cells and progenitor cells [2].
In vitro, Cyclosporin H (1 μM) treated A549 cells for 30 min and strongly inhibited mitochondrial DAMP-induced IL-8 release in cells [1]. Cyclosporin H (8μM) treated mouse hematopoietic progenitor cells and stem cells for 24 hours, significantly improving the efficiency of cellular lentiviral transduction [3]. Cyclosporin H (8-800 nM) treats N-formyl-methionine-leucine-phenylalanine (FMLP)-activated basophils and concentration-dependently inhibits the release of histamine and leukotriene C4 from cells[4].
In vivo, Cyclosporin H (2mg/kg) treated lung injury model mice through intravenous injection, reduced the entry of neutrophils into the alveolar space, inhibited the levels of inflammatory factors in the bronchoalveolar lavage fluid, and improved lung morphological damage [5]. Cyclosporin H (30mg/kg) treated middle cerebral artery occlusion (MCAO) model mice through intravenous injection, alleviated ischemic cerebral infarction and inhibited neutrophil infiltration [6]. Cyclosporin H (30 mg/kg), administered intraperitoneally to breast cancer mice, produced an immunosuppressive effect and reduced the efficacy of chemotherapy with mitoxantrone (MTX) and cyclophosphamide (CTX) [7].
References:
[1] Wenzel-Seifert K, Seifert R. Cyclosporin H is a potent and selective formyl peptide receptor antagonist. Comparison with Nt-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L-leucyl-L-phenylalanine and cyclosporins A, B, C, D, and E[J]. Journal of immunology, 1993, 150: 4591-4599.
[2] Petrillo C, Thorne L G, Unali G, et al. Cyclosporine H overcomes innate immune restrictions to improve lentiviral transduction and gene editing in human hematopoietic stem cells[J]. Cell Stem Cell, 2018, 23(6): 820-832. e9.
[3] Olender L, Bujanover N, Sharabi O, et al. Cyclosporine H improves the multi-vector lentiviral transduction of murine haematopoietic progenitors and stem cells[J]. Scientific Reports, 2020, 10(1): 1812.
[4] 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]. Journal of allergy and clinical immunology, 1996, 98(1): 152-164.
[5] Zhang X, Wang T, Yuan Z C, et al. Mitochondrial peptides cause proinflammatory responses in the alveolar epithelium via FPR-1, MAPKs, and AKT: a potential mechanism involved in acute lung injury[J]. American Journal of Physiology-Lung Cellular and Molecular Physiology, 2018, 315(5): L775-L786.
[6] Hong Z, Xu H, Ni K, et al. Effect of Cyclosporin H on ischemic injury and neutrophil infiltration in cerebral infarct model of rats via PET imaging[J]. Annals of Nuclear Medicine, 2024: 1-13.
[7] Baracco E E, Pietrocola F, Buqué A, et al. Inhibition of formyl peptide receptor 1 reduces the efficacy of anticancer chemotherapy against carcinogen-induced breast cancer[J]. Oncoimmunology, 2016, 5(6): e1139275.
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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