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.

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 K_i 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 K_i 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 K_i values of 0.08, 0.24, and 0.45 μM, respectively^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1202.61

C₆₂H₁₁₁N₁₁O₁₂

83602-39-5

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)}]

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

Room temperature in continental US; may vary elsewhere.

Powder	-80deg;C	2 years
	-20deg;C	1 year
In solvent	-80deg;C	6 months
	-20deg;C	1 month

In Vitro:;

DMSO : 100 mg/mL (83.15 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

  Solubility: 3 mg/mL (2.49 mM); Suspended solution; Need ultrasonic

  此方案可获得 3 mg/mL (2.49 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

  Solubility: 3 mg/mL (2.49 mM); Suspended solution; Need ultrasonic

  此方案可获得 3 mg/mL (2.49 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

  Solubility: ≥ 2.5 mg/mL (2.08 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (2.08 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.