Cyclosporin H (Synonyms: 5-(N-methyl-D-valine)-Cyclosporin A, Sandoz 37-839) |
| Catalog No.GC15319 |
Cyclosporin H는 강력하고 선택적인 폼릴 펩티드 수용체(FPR) 앙티아고니스트로, IC50 값이 0.7μM이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 83602-39-5
Sample solution is provided at 25 µL, 10mM.
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Cyclosporin H는 강력하고 선택적인 폼릴 펩티드 수용체(FPR) 앙티아고니스트로, IC50 값이 0.7μM이다.
Cyclosporin H는 바이러스 운반 강화제로 사용되어 혈포성 스템 셀 및 선구세포에서 렌티바이럴 운반의 효율성을 향상시킬 수 있다[2].
체외 실험에서 Cyclosporin H (1μM)은 A549 세포에 30분 동안 처리되어 미토콘드릴 DAMP 유도 IL-8의 세포 내 방출을 강력하게 억제하였다[1]. Cyclosporin H (8μM)은 24시간 동안 쥐 혈포생 선구세포 및 스템세포에 처리되어 렌티바이럴 운반 효율성을 크게 향상시켰다[3]. Cyclosporin H (8-800nM)은 N-포믈메티오닌-레우시네-페닐알라닌(FMLP) 활성화된 세포에 처리되어 세포 내의 히스타민 및 루코트리에늄 C4 방출을 농도에 따라 억제하였다[4].
체내 실험에서 Cyclosporin H(2mg/kg)은 정맥 주입을 통한 폐 손상 모델 쥐에 투여되어 중성 백혈구가 푹실 공간으로 들어가는 것을 감소시켰으며, 기관지 폐포물에 있는 염증 인자 수준을 억제하고 폐의 모양학적 손상을 개선했다[5]. Cyclosporin H(30mg/kg)은 정맥 주입을 통한 중풍 모델 쥐에 투여되어 뇌경색을 완화시키고 중성 백혈구 침투를 억제했다[6]. Cyclosporin H(30 mg/kg)은 복강 주입을 통한 유방암 쥐에 투여되어 면역억제 효과를 일으키고, mitoxantrone (MTX)과 cyclophosphamide (CTX)의 화학 요법 효과를 감소시켰다[7].
References:
[1] Wenzel-Seifert K, Seifert R. Cyclosporin H is a potent and selective formyl peptide receptor antagonist. Comparison with Nt-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L-leucyl-L-phenylalanine and cyclosporins A, B, C, D, and E[J]. Journal of immunology, 1993, 150: 4591-4599.
[2] Petrillo C, Thorne L G, Unali G, et al. Cyclosporine H overcomes innate immune restrictions to improve lentiviral transduction and gene editing in human hematopoietic stem cells[J]. Cell Stem Cell, 2018, 23(6): 820-832. e9.
[3] Olender L, Bujanover N, Sharabi O, et al. Cyclosporine H improves the multi-vector lentiviral transduction of murine haematopoietic progenitors and stem cells[J]. Scientific Reports, 2020, 10(1): 1812.
[4] de Paulis A, Ciccarelli A, de Crescenzo G, et al. Cyclosporin H is a potent and selective competitive antagonist of human basophil activation by N-formyl-methionyl-leucyl-phenylalanine[J]. Journal of allergy and clinical immunology, 1996, 98(1): 152-164.
[5] Zhang X, Wang T, Yuan Z C, 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[J]. American Journal of Physiology-Lung Cellular and Molecular Physiology, 2018, 315(5): L775-L786.
[6] Hong Z, Xu H, Ni K, et al. Effect of Cyclosporin H on ischemic injury and neutrophil infiltration in cerebral infarct model of rats via PET imaging[J]. Annals of Nuclear Medicine, 2024: 1-13.
[7] Baracco E E, Pietrocola F, Buqué A, et al. Inhibition of formyl peptide receptor 1 reduces the efficacy of anticancer chemotherapy against carcinogen-induced breast cancer[J]. Oncoimmunology, 2016, 5(6): e1139275.
세포 실험 [1]: | |
세포 라인 | 쥐 혈액 생성 조상 및 간세포 |
제조 방법 | Cyclosporin H(최종 농도 8µM) 또는 DMSO가 세포 분류 직후에 첨가되었으며, 펄스레이션 후 제거되었다. 세포를 촘촘히 회전시켜 중첩시켰고 매질을 Cyclosporin H 또는 DMSO를 포함하는 신선한 매질로 교체했으며, 이러한 화합물이 존재하는 상황에서 세포를 추가 24시간 배양한 후 치명적으로 방사선을 받은 수용체에 이식하였다. |
반응 조건 | 8μM; 24 h |
응용 분야 | Cyclosporin H는 쥐 혈액 생성 조상 및 간세포의 다중 벡터 렌티바이럴 펄스레이션 효율성을 향상시킨다. |
동물 실험 [2]: | |
동물 모형 | BALB/c 쥐 |
제조 방법 | 쥐는 무작위로 6개 그룹으로 나뉘어졌다 (각 시간점에서 그룹당 4-6마리): Hank’s Balanced Salt Solution (HBSS)을 기관 내투여로 받는 통제 그룹 (MTDs/fMLP), 꼬리 혈관을 통하여 2mg/kg의 Cyclosporin H를 투여받는 투여하는 Cyclosporin H 군으로 나누었다. |
제형 | 2 mg/kg; i.v. |
응용 분야 | Cyclosporin H는 MTDs 또는 fMLP 도전으로 인한 쥐의 폐 손상을 현저하게 완화시킬 수 있다. |
참고문헌: [1]Olender L, Bujanover N, Sharabi O등. Cyclosporin H는 머린 조혈모세포 원자와 줄기 세포의 다중 벡터 렌티바이러스 변환을 향상시킨다 [J].Scientific Reports, 2020, 10(1):1812. [2] Zhang X, Wang T, Yuan Z C등.미토콘드리아 펩타이드는 FPR-1, MAPKs 및 AKT를 통해 폐포상피에서 proinflammatory 반응을 일으킨다:급성 폐손상에 관여하는 잠재적 기전 [J].American Journal of Physiology-Lung cell and Molecular Physiology, 2018, 315(5):L775-L786. | |
| Cas No. | 83602-39-5 | SDF | |
| Synonyms | 5-(N-methyl-D-valine)-Cyclosporin A, Sandoz 37-839 | ||
| Chemical Name | (3R,6S,9S,12R,13Z,15S,16Z,18S,21S,22Z,24S,30S,31E,33S)-30-ethyl-14,17,23,32-tetrahydroxy-33-((1R,2R,E)-1-hydroxy-2-methylhex-4-en-1-yl)-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacycl | ||
| Canonical SMILES | C/C([H])=C([H])/C[C@@]([C@](O)([H])[C@@](N1C)([H])/C(O)=N\[C@@](C(N(CC(N([C@@](/C(O)=N/[C@@](C(N([C@@](/C(O)=N/[C@@](/C(O)=N/[C@](C(N([C@@](C(N([C@@](C(N([C@](C1=O)([H])C(C)C)C)=O)([H])CC(C)C)C)=O)([H])CC(C)C)C)=O)([H])C)([H])C)([H])CC(C)C)C)=O)([H])C(C)C | ||
| Formula | C62H111N11O12 | M.Wt | 1202.61 |
| Solubility | Chloroform: Slightly Soluble,Methanol: Slightly Soluble; DMSO: 100 mg/mL (83.15 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 831.5 μL | 4.1576 mL | 8.3152 mL |
| 5 mM | 166.3 μL | 831.5 μL | 1.663 mL |
| 10 mM | 83.2 μL | 415.8 μL | 831.5 μL |
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