Cyclosporin H (Synonyms: 5-(N-methyl-D-valine)-Cyclosporin A, Sandoz 37-839) |
| Catalog No.GC15319 |
Cyclosporin H is a potent and selective formyl peptide receptor (FPR) antagonist with an IC50 value of 0.7μM.
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.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Cyclosporin H is a potent and selective formyl peptide receptor (FPR) antagonist with an IC50 value of 0.7μM[1]. Cyclosporin H can be used as a viral transduction enhancer to improve the efficiency of lentiviral transduction in hematopoietic stem cells and progenitor cells [2].
In vitro, Cyclosporin H (1 μM) treated A549 cells for 30 min and strongly inhibited mitochondrial DAMP-induced IL-8 release in cells [1]. Cyclosporin H (8μM) treated mouse hematopoietic progenitor cells and stem cells for 24 hours, significantly improving the efficiency of cellular lentiviral transduction [3]. Cyclosporin H (8-800 nM) treats N-formyl-methionine-leucine-phenylalanine (FMLP)-activated basophils and concentration-dependently inhibits the release of histamine and leukotriene C4 from cells[4].
In vivo, Cyclosporin H (2mg/kg) treated lung injury model mice through intravenous injection, reduced the entry of neutrophils into the alveolar space, inhibited the levels of inflammatory factors in the bronchoalveolar lavage fluid, and improved lung morphological damage [5]. Cyclosporin H (30mg/kg) treated middle cerebral artery occlusion (MCAO) model mice through intravenous injection, alleviated ischemic cerebral infarction and inhibited neutrophil infiltration [6]. Cyclosporin H (30 mg/kg), administered intraperitoneally to breast cancer mice, produced an immunosuppressive effect and reduced the efficacy of chemotherapy with mitoxantrone (MTX) and cyclophosphamide (CTX) [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.
Cell experiment [1]: | |
Cell lines | murine haematopoietic progenitors and stem cells |
Preparation method | Cyclosporin H (final concentration 8µM) or DMSO was added immediately after cell sorting and removed after transduction. Following centrifugation, the medium was replaced with fresh medium containing Cyclosporin H or DMSO, and the cells were incubated for an additional 24 hours in the presence of these compounds prior to transplantation into lethally irradiated recipients. |
Reaction Conditions | 8μM; 24 h |
Applications | Cyclosporine H improves the multi-vector lentiviral transduction of murine haematopoietic progenitors and stem cells. |
Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation method | mice were randomly divided into 6 groups (n=4-6/group at each time point): control group (MTDs/fMLP) receiving Hank’s Balanced Salt Solution (HBSS) intratracheally, Cyclosporin H group receiving 2 mg/kg of Cyclosporin H by tail vein. |
Dosage form | 2 mg/kg; i.v. |
Applications | Cyclosporin H could significantly attenuate lung injury in MTDs or fMLP-challenged mice. |
References: [1]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. [2]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. | |
| 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 | 0.8315 mL | 4.1576 mL | 8.3152 mL |
| 5 mM | 0.1663 mL | 0.8315 mL | 1.663 mL |
| 10 mM | 0.0832 mL | 0.4158 mL | 0.8315 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *