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Cyclosporin A Immunosuppressive agent

Catalog No.B1922
Size Price Stock Qty
10mM (in 1mL DMSO)
$55.00
In stock
100mg
$50.00
In stock
200mg
$70.00
In stock
500mg
$100.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Yang YL, Li J, et al. "Ginsenoside Rg5 increases cardiomyocyte resistance to ischemic injury through regulation of mitochondrial hexokinase-II and dynamin-related protein 1." Cell Death Dis. 2017 Feb 23;8(2):e2625. PMID:28230856

Quality Control

Chemical structure

Cyclosporin A

Related Biological Data

Cyclosporin A

Protocol

Cell experiment [1]:

Cell lines

Jurkat T cells and A549 lung carcinoma cells

Preparation method

The solubility of this compound in DMSO is >60.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 μM, 24h

Applications

Pretreatment of fresh T cells with CsA during primary TCR stimulation decreased their production of TGF-β1 during secondary stimulation. Higher concentrations of CsA (10 μM) promoted the release of preformed TGF-β1 by inducing apoptosis.

Animal experiment [2]:

Animal models

Female retinal ischemia C57BL/6 mouse model

Dosage form

Intraperitoneal injection, 5 mg/kg per day

Application

CsA significantly promoted RGC survival in ischemic retina. CsA treatment significantly decreased GFAP and CypD protein expression in ischemic retina at 12 h. CsA treatment decreased CypD immunoreactivity in the inner layer of ischemic retina.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Minguillón J, Morancho B, Kim S J, et al. Concentrations of cyclosporin A and FK506 that inhibit IL-2 induction in human T cells do not affect TGF-β1 biosynthesis, whereas higher doses of cyclosporin A trigger apoptosis and release of preformed TGF-β1[J]. Journal of leukocyte biology, 2005, 77(5): 748-758.

[2]. Kim S Y, Shim M S, Kim K Y, et al. Inhibition of cyclophilin D by cyclosporin A promotes retinal ganglion cell survival by preventing mitochondrial alteration in ischemic injury[J]. Cell death & disease, 2014, 5(3): e1105.

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Chemical Properties

Cas No. 59865-13-3 SDF Download SDF
Canonical SMILES CCC1C(=O)N(CC(=O)N(C(C(=O)NC(C(=O)N(C(C(=O)NC(C(=O)NC(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N(C(C(=O)N1)C(C(C)CC=CC)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C
Formula C62H111N11O12 M.Wt 1202.61
Solubility >60.2mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Cyclosporin A is a selective cyclophilin inhibitor with IC50 value of 7 nM [1].

Cyclophilins are isomerase enzymes and involve in a variety of functions related to cell metabolism and energy homeostasis. It has been reported that the over expression of cyclophilins were observed in inflammation or malignancy.

Cyclosporin A is a potent cyclophilin inhibitor which is responsible for the opening of the MPTP (mitochondrial permeability transition pore). When tested with retinal ganglion cells, Cyclosporin A showed a high selectivity for the expression of cyclophilin D and prolonged the cells survival [2]. In human First-Trimester Trophoblast Cells, Cyclosporin A treatment promoted cells growth and invasiveness by inhibiting Ca2+/Calcineurin/NFAT signal [3]. Cyclosporin A treatment promoted the apoptosis of T-cell by upregulating Fas/FasL and caspase activities [4]. Treated human T cells with Cyclosporin A suppressed T cell activation by inhibiting calcineurin and NFATc which are responsible for T cell function [1].

In retinal ischemia C57BL/6 mouse model, Cyclosporin A treatment significantly prevented the up regulation of cyclophilin D and ameliorated the death of neuronal cells in vivo [2].

Cyclosporin A has also been reported to inhibit the entry of hepatitis B and C virus through interfering NTCP reportor [5]. In CRC cell lines (CACO-2, HT-29, HCT-116 and LOVO), Cyclosporin A treatment also could impair cell growth via without calcineurin pathway while the mechanism was still undermined [6].

References:
[1].  Minguillon, J., et al., Concentrations of cyclosporin A and FK506 that inhibit IL-2 induction in human T cells do not affect TGF-beta1 biosynthesis, whereas higher doses of cyclosporin A trigger apoptosis and release of preformed TGF-beta1. J Leukoc Biol, 2005. 77(5): p. 748-58.
[2].  Kim, S.Y., et al., Inhibition of cyclophilin D by cyclosporin A promotes retinal ganglion cell survival by preventing mitochondrial alteration in ischemic injury. Cell Death Dis, 2014. 5: p. e1105.
[3].  Du, M.R., et al., Cyclosporin A promotes growth and invasiveness in vitro of human first-trimester trophoblast cells via MAPK3/MAPK1-mediated AP1 and Ca2+/calcineurin/NFAT signaling pathways. Biol Reprod, 2008. 78(6): p. 1102-10.
[4].  Gao, J., et al., Mitochondrial permeability transition pore in inflammatory apoptosis of human conjunctival epithelial cells and T cells: effect of cyclosporin A. Invest Ophthalmol Vis Sci, 2013. 54(7): p. 4717-33.
[5].  Nkongolo, S., et al., Cyclosporin A inhibits hepatitis B and hepatitis D virus entry by cyclophilin-independent interference with the NTCP receptor. J Hepatol, 2014. 60(4): p. 723-31.
[6].  Werneck, M.B., et al., Cyclosporin A inhibits colon cancer cell growth independently of the calcineurin pathway. Cell Cycle, 2012. 11(21): p. 3997-4008.