| Description | 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. |
| In vitro | Cyclosporin H是一种强效的抑制剂，能抑制FMLP诱导的超氧阴离子(O2-)在人类中性粒细胞中的生成。在HL-60膜中，Cyclosporin H以0.10 μM的Ki（抑制常数）抑制了FMLP的结合。此外，Cyclosporin H还通过0.79 μM的Ki值抑制了于HL-60膜中FMLP对高亲和力GTP酶（异源三聚体调节性鸟苷核苷酸结合蛋白的α亚单位的酶活性）的激活。Cyclosporin H对FMLP对细胞内Ca2+浓度（[Ca2+]i）、O2-生成和β-葡萄糖醛酸酶释放的刺激效应，分别以0.08、0.24、和0.45 μM的Ki值进行了抑制。 |
| In vivo | 环孢素H（5 mg/kg；腹腔注射；在LPS或HCl挑战前）可减轻由LPS或HCl（一种肺损伤模型）引起的肺损伤。 |
| Target activity | FMLP:0.1 μM (ki) |
| molecular weight | 1202.61 |
| Molecular formula | C62H111N11O12 |
| CAS | 83602-39-5 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 99 mg/mL (82.32 mM) |
| References | 1. Zhang X, 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. Am J Physiol Lung Cell Mol Physiol. 2018;315(5):L775-L786. 2. Wenzel-Seifert K, et al. 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. |