MedChemExpress - Model Cyclosporin H -83602-39-5

Cyclosporin H is a selective and potent inhibitor of FPR-1 (formyl peptide receptor 1). Cyclosporin H, a viral transduction enhancer, increases lentiviral transduction up to 10-fold in human cord blood-derived hematopoietic stem and progenitor cells (HSPCs). Cyclosporin H displays an additive effect when combined with Rapamycin (HY-10219) or Prostaglandin E2 (HY-101952). Cyclosporin H lacks immunosuppressant activity of Cyclosporin A.

Cyclosporin H

MCE China：Cyclosporin H

Brand：MedChemExpress (MCE)

Cat. No.HY-P1122

CAS：83602-39-5

Purity：99.43%

Storage：Sealed storage, away from moisture Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Cyclosporin H is a selective and potent inhibitor of FPR-1 (formyl peptide receptor 1). Cyclosporin H, a viral transduction enhancer, increases lentiviral transduction up to 10-fold in human cord blood-derived hematopoietic stem and progenitor cells (HSPCs). Cyclosporin H displays an additive effect when combined with Rapamycin (HY-10219) or Prostaglandin E2 (HY-101952). Cyclosporin H lacks immunosuppressant activity of Cyclosporin A.

In Vitro：The cyclic undecapeptide, cyclosporin H, is a potent inhibitor of formyl-Met-Leu-Phe (FMLP)-induced superoxide anion (O2-) formation in human neutrophils. Cyclosporin H inhibits FMLP binding in HL-60 membranes with a Ki of 0.1 μM. Cyclosporin H inhibits 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 inhibits 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[2].

In Vivo：Cyclosporin H (5 mg/kg; i.p.; before LPS or HCl challenge) attenuats lung injury induced by LPS or HCl (a lung injurymodel)[1].

Sequence：Cyclo[{Abu}-{Sar}-{N(Me)Leu}-Val-{N(Me)Leu}-Ala-{d-Ala}-{N(Me)Leu}-{N(Me)Leu}-{d-N(Me)Val}-{N(Me)Bmt(E)}]

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. [Content Brief]

[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. [Content Brief]

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MedChemExpress - Model Cyclosporin H -83602-39-5

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Cyclosporin H