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Submit ReviewCyclosporin A is an immunosuppressant; simultaneously binds calcineurin and cyclophilin and inhibits phosphatase activity of calcineurin (IC50 = 5 nM). Additionally inhibits formation and opening of the mitochondrial permeability transition pore (MPTP). Also inhibits coronavirus replication in vitro. Enhances lentirival transduction of bone marrow-derived CD34+ cells and is additive with Prostaglandin E2 (Cat. No. 2296).
Cyclosporin A is also offered as part of the Tocriscreen Antiviral Library, Tocriscreen Epigenetics Library and Tocriscreen Stem Cell Library. 了解 Tocris 化合物库的更多信息。
分子量 | 1202.63 |
公式 | C62H111N11O12 |
储存 | Store at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 59865-13-3 |
PubChem ID | 2909 |
InChI Key | PMATZTZNYRCHOR-CGLBZJNRSA-N |
Smiles | [H][C@@]1(C(C)C)NC([C@@H](N(C(CN(C([C@@H](NC([C@]([C@@H]([C@@H](C/C=C/C)C)O)(N(C([C@](C(C)C)(N(C([C@@H](N(C([C@](CC(C)C)(N(C([C@H](NC([C@@H](NC([C@@H](N(C1=O)C)CC(C)C)=O)C)=O)C)=O)C)[H])=O)C)CC(C)C)=O)C)[H])=O)C)[H])=O)CC)=O)C)=O)C)CC(C)C)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 120.26 | 100 | |
ethanol | 60.13 | 50 |
以下数据基于产品分子量 1202.63。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 0.83 mL | 4.16 mL | 8.32 mL |
5 mM | 0.17 mL | 0.83 mL | 1.66 mL |
10 mM | 0.08 mL | 0.42 mL | 0.83 mL |
50 mM | 0.02 mL | 0.08 mL | 0.17 mL |
参考文献是支持产品生物活性的出版物。
Brookemeier and Pfeiffer (1995) Inhibition of the mitochondrial permeability transition pore by cyclosporin A during long time frame experiments: relationship between pore opening and the activity of mitochondrial phospholipases. Biochemistry 34 16440 PMID: 8845372
Fruman et al (1992) Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc.Natl.Acad.Sci.U.S.A. 89 3686 PMID: 1373887
Nakata et al (1998) Evidence that cyclosporin A and dexameth. inhibit allergic airway inflammation via suppression of interleukin-5 synthesis by T cells. Br.J.Pharmacol. 124 1425 PMID: 9723954
Yan et al (2009) Cyclosporin-A potently induces highly cardiogenic progenitors from embryonic stem cells. Biochem.Biophys.Res.Commun. 379 115 PMID: 19094963
Petrillo et al (2019) Assessing the impact of cyclosporin A on lentiviral transduction and preservation of human hematopoietic stem cells in clinically relevant ex vivo gene therapy settings. Hum.Gene.Ther. 30 1133 PMID: 31037976
de Wilde et al (2011) Cyclosporin A inhibits the replication of diverse coronaviruses. J.Gen.Virol. 92 2542 PMID: 21752960
de Wilde et al (2013) MERS-coronavirus replication induces severe in vitro cytopathology and is strongly inhibited by cyclosporin A or interferon-α treatment. J.Gen.Virol. 94 1749 PMID: 23620378
Carbajo-Lozoya et al (2014) Human coronavirus NL63 replication is cyclophilin A-dependent and inhibited by non-immunosuppressive cyclosporine A-derivatives including Alisporivir. Virus Res. 184 44 PMID: 24566223
If you know of a relevant reference for Cyclosporin A, please let us know.
关键词: Cyclosporin A, Cyclosporin A supplier, Calcineurin, inhibitors, Protein, Ser/Thr, Phosphatases, CyclosporinA, immunosuppressant, CsA, inhibits, mPTP, mitochondrial, permeability, transition, pore, antibiotics, coronaviruses, SARS-CoV, severe, acute, respiratory, syndrome, COVID-19, MERS, cyclophilin, PPI, peptidylprol, Ciclosporin, A, Immunosuppressants, MPTP, NFAT, Viral, Transduction, Enhancers, Other, Isomerases, Coronavirus, 1101, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Cyclosporin A 的部分引用包括:
Cui et al (2016) Endocannabinoid dynamics gate spike-timing dependent depression and potentiation. Elife 5 e13185 PMID: 26920222
Palmqvist et al (2016) A human and animal model-based approach to investigating the anti-inflammatory profile and potential of the 5-HT2B receptor antagonist AM1030. J Inflamm (Lond) 13 20 PMID: 27340371
Liu et al (2015) Hyperphosphate-Induced Myocardial Hypertrophy through the GATA-4/NFAT-3 Signaling Pathway Is Attenuated by ERK Inhibitor Treatment. Exp Eye Res 5 79 PMID: 25999956
Faralli et al (2015) NFATc1 activity regulates the expression of myocilin induced by dexameth. J Biol Chem 130 42614 PMID: 25450062
Draganov et al (2015) Modulation of P2X4/P2X7/Pannexin-1 sensitivity to extracellular ATP via iverm. induces a non-apoptotic and inflammatory form of cancer cell death. J Neurosci 5 16222 PMID: 26552848
Gray et al (2014) Inhibitory interactions between phosphorylation sites in the C terminus of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-type glutamate receptor GluA1 subunits. Mol Immunol 289 14600 PMID: 24706758
Battefeld et al (2019) High-Frequency Microdomain Ca2+ Transients and Waves during Early Myelin Internode Remodeling. Cell Rep 26 182 PMID: 30605675
Agarwal et al (2017) Transient Opening of the Mitochondrial Permeability Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes. Neuron 93 587 PMID: 28132831
Li and Burrell (2011) Associative, bidirectional changes in neural signaling utilizing NMDA receptor- and endocannabinoid-dependent mechanisms. Learn Mem 18 545 PMID: 21844187
George et al (2011) Calcium-dependent phosphorylation regulates neuronal stability and plasticity in a highly precise pacemaker nucleus. J Neurophysiol 106 319 PMID: 21525377
O'Donnell et al (2016) Transient Oxygen/Glucose Deprivation Causes a Delayed Loss of Mitochondria and Increases Spontaneous Calcium Signaling in Astrocytic Processes. J Neurosci 36 7109 PMID: 27383588
Grodzki et al (2009) FcεRI-induced activation by low antigen concentrations results in nuclear signals in the absence of degranulation. PLoS One 46 2539 PMID: 19540596
Panja et al (2019) Paraneoplastic cerebellar degeneration: Yo antibody alters mitochondrial calcium buffering capacity. Neuropathol Appl Neurobiol 45 141 PMID: 29679372
Miyamoto et al (2016) Increasing the Receptor Tyrosine Kinase EphB2 Prevents Amyloid-β-induced Depletion of Cell Surface Glutamate Receptors by a Mechanism That Requires the PDZ-binding Motif of EphB2 and Neuronal Activity. Cardiorenal Med 291 1719 PMID: 26589795
Bhosale and Duchen (2019) Investigating the Mitochondrial Permeability Transition Pore in Disease Phenotypes and Drug Screening. Curr Protoc Pharmacol e59 PMID: 31081999
Puri et al (2019) Mul1 restrains Parkin-mediated mitophagy in mature neurons by maintaining ER-mitochondrial contacts. Nat Commun 10 3645 PMID: 31409786
Piccart et al (2015) Neurotensin Induces Presynaptic Depression of D2 DA Autoreceptor-Mediated Neurotransmission in Midbrain DArgic Neurons. J Neurosci 35 11144 PMID: 26245975
Lopez et al (2022) Ketamine exerts its sustained antidepressant effects via cell-type-specific regulation of Kcnq2. Neuron 110 2283 PMID: 35649415
Belmeguenai and Hansel (2005) A role for protein phosphatases 1, 2A, and 2B in cerebellar long-term potentiation. J Biol Chem 25 10768 PMID: 16291950
Ceglia et al (2010) Signaling pathways controlling the phosphorylation state of WAVE1, a regulator of actin polymerization. J Neurochem 114 182 PMID: 20403076
Pérez et al (2018) Mitochondrial permeability transition pore contributes to mitochondrial dysfunction in fibroblasts of patients with sporadic Alzheimer's disease. Redox Biol 19 290 PMID: 30199818
Burdyga et al (2018) Phosphatases control PKA-dependent functional microdomains at the outer mitochondrial membrane. Proc Natl Acad Sci U S A. 115 E6497 PMID: 29941564
Yu et al (2014) Differential effects of the Toll-like receptor 2 agonists, PGN and Pam3CSK4 on anti-IgE induced human mast cell activation. PLoS One 9 e112989 PMID: 25398056
Gross et al (2013) Roles of endothelial nitric oxide synthase (eNOS) and mitochondrial permeability transition pore (MPTP) in epoxyeicosatrienoic acid (EET)-induced cardioprotection against infarction in intact rat hearts. J Mol Cell Cardiol 59 20 PMID: 23419451
Pont et al (2012) Oxytocin-stimulated NFAT transcriptional activation in human myometrial cells. Mol.Endocrinol. 26 1743 PMID: 22902539
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Used cyclosporin as a natural control to understand few other synthetic immunosuppressants.