Cyclosporin H 是一种 FPR-1(甲酰肽受体 1) 的选择性强效抑制剂。它缺乏 Cyclosporin A 具有的免疫抑制活性。它是一种病毒转导增强剂，可使人脐带血来源的造血干细胞和祖细胞中慢病毒转导增强 10 倍。它与雷帕霉素或前列腺素 E2 联合使用时表现出累加效应。

Cyclosporin H (CsH), a specific inhibitor of FPR1, inhibited lung inflammation in the ALI models. CsH significantly attenuated MTDs or NFP-induced inflammatory lung injury and activation of MAPK and AKT pathways. Cyclosporin H is a viral transduction enhancer which increases lentiviral transduction up to 10-fold in human cord blood-derived hematopoietic stem and progenitor cells (HSPCs). When combined with Rapamycin or Prostaglandin E2 Cyclosporin H displays an additive effect. Cyclosporin H lacks immunosuppressant activity of Cyclosporin A.

Cyclosporin H is a potent inhibitor of FMLP-induced superoxide anion (O2-) formation in human neutrophils. Cyclosporin H inhibited FMLP binding in HL-60 membranes with a Ki (inhibition constant) of 0.10 μM. Cyclosporin H inhibited activation by FMLP of high affinity GTPase (the enzymatic activity of alpha-subunits of heterotrimeric regulatory guanine nucleotide-binding proteins) in HL-60 membranes with a Ki of 0.79 μM. Cyclosporin H inhibited the stimulatory effects of FMLP on cytosolic Ca2+ concentration ([Ca2+]i), O2- formation, and beta-glucuronidase release with Ki values of 0.08, 0.24, and 0.45 μM, respectively.

Cyclosporin H (5 mg/kg; i.p.; before LPS or HCl challenge) weakens lung injury induced by LPS or HCl (a lung injurymodel).

83602-39-5

C62H111N11O12

1202.61

DMSO:99 mg/mL (82.32 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years