CAS:83602-39-5Cyclosporin H

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Cyclosporin H is a potent and effective inhibitor of formyl peptide receptor (FPR) with Ki of 0.1 uM.

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18817579266

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描述As an initial signal in the innate immunity, the formyl peptide stimulates leukocyte chemotaxis, induces acute and chronic inflammation, and stimulates the release of a number of the cytokine storm mediators from monocytes, neutrophils and endothelial cells by acting through the formyl peptide receptor (FPR). Cyclosporin H, a potent anti-inflammatory compound, acts as a specific competitive antagonist of formyl peptides on FPR on phagocytic: leukocytes. Cyclosporin H completely blocked neutrophil chemotaxis induced by the standard formyl peptide, f-MLF, as well as the bacteria-derived or host-derived formyl peptide^[1]. Cyclosporin H (8 to 800 nM) concentration-dependently inhibited histamine and leukotriene C4 release from purified and unpurified basophils activated by FMLP. Furthermore, Cyclosporin H inhibited tritiated FMLP binding to human polymorphonuclear leukocytes with a concentration required to inhibit binding by 50% of approximately 0.54 nM^[2]. In vivo treatment by Cyclosporin H in the mouse model of HINI Swine flu influenza infection for 5 days markedly reduced lung inflammation and endothelial cell damage^[1].