Cyclosporin A

For research use only.

Catalog No.S2286 Synonyms: Cyclosporine A

32 publications

Cyclosporin A  Chemical Structure

CAS No. 59865-13-3

Cyclosporin A (Cyclosporine A) is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, widely used in organ transplantation to prevent rejection.

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Selleck's Cyclosporin A has been cited by 32 publications

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Biological Activity

Description Cyclosporin A (Cyclosporine A) is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, widely used in organ transplantation to prevent rejection.
Targets
calcineurin [1]
(Cell-free assay)
7 nM
In vitro

Cyclosporin A binds to the cyclophilin (immunophilin) in T cells[1] , forms a Cyclophilin-Cyclosporin A complex which the binds to and inhibits calcineurin. [2] Cyclosporin A inhibits calcineurin with IC50 of 7 nM[3], then blocks the nuclear translocation of NF-AT. [4] Cyclosporin A also affects mitochondria by preventing the MTP (mitochondrial permeability transition pore) from opening with an IC50 of 39 nM. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 cells M17VPGZ2dmO2aX;uJIF{e2G7 M{SxSWlvcGmkaYTpc44hd2ZibHn2[ZIhe3SjZ3WgVIxie22xZHn1cUBj\XKpaHXpJIlv\mWldHnvckBqdiCKZYDHNkBk\WyuczygTWM2OD1zLk[1JI5O NWnOeZhuOjJ3OE[xNlQ>
Jurkat cells MUnGeY5kfGmxbjDhd5NigQ>? Mni3TY1ufW6xc4XwdJJme3OrdnWgZYN1cX[rdImge4F{KG2nYYP1doVlKGK7IHnubIljcXSrb36gc4YhfGinIFnMMVIheHKxZIXjeIlwdiCrbjDKeZJs[XRiY3XscJMtKEmFNUC9NkBvVQ>? M4XlOlE1PjR|M{O3
human PBMC MX;GeY5kfGmxbjDhd5NigQ>? NYW0TFFwOSCq NXvJTWJPSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCqdX3hckBRSk2FIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYX70bU1ETDNxQ1SyPEBidnSrYn;kfU1qdmS3Y3XkJGlNNTJicILv[JVkfGmxbjD0doVifGWmIH\vdkAyKGi{IHLl[o9z\SCjboTpMWNFOy:FREK4JIFvfGmkb3T5JINp[WyuZX7n[UBu\WG|dYLl[EBi\nSncjC2JIhzeyCkeTDpcY12dm:|dYDwdoV{e2mxbjDhd5NigSxiRVO1NF0{NjFibl2= MlvGNVk6OzN5OUW=
human Jurkat cells MXPGeY5kfGmxbjDhd5NigQ>? MkDYNUBp NWDsOlFySW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCqdX3hckBLfXKtYYSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjboTpMWNFOy:FREK4JIFvfGmkb3T5MYlv\HWlZXSgTWwuOiCycn;keYN1cW:wIITy[YF1\WRiZn;yJFEhcHJiYnXmc5JmKGGwdHmtR2Q{N0OGMkigZY51cWKxZImgZ4hidGynbnflJI1m[XO3cnXkJIFnfGW{IE[gbJJ{KGK7IHntcZVvd3O3cIDy[ZN{cW:wIHHzd4F6NCCHQ{WwQVUhdk1? NW\1OWoyOTl7M{O3PVU>
human T-cell MlP4SpVv[3Srb36gZZN{[Xl? Ml3UTY4hfmm2cn:gbY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGStZ4VtdCCycn;keYN1cW:wIH;mJIx6dXCqb3vpcoUhUUxvMjygTWM2OD16LkGgcm0> NGrLWXc4PTN5M{Ox
human splenocytes MWHGeY5kfGmxbjDhd5NigQ>? M{HPZlQh\GG7cx?= Ml70TY1ufW6xc4XwdJJme3OrdnWgZYN1cX[rdImgbY4hcHWvYX6gd5Bt\W6xY4n0[ZMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBcO0ifdHj5cYllcW6nIHnuZ49zeG:{YYTpc44h[W[2ZYKgOEBl[Xm|IHL5JIFtdG:pZX7pZ{BucXinZDDsfY1xcG:leYTlJJJm[WO2aX;uJIF{e2G7LDDJR|UxRTFyIH7N NVfUZlE5OTl6Mke4N|E>
mouse T cells NX\aT4VuTnWwY4Tpc44h[XO|YYm= MXe0JIRigXN? MlX6TY1ufW6xc4XwdJJme3OrdnWgZYN1cX[rdImgbY4hdW:3c3WgWEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIIT3c{B4[XlibXn4[YQhdHmvcHjvZ5l1\SC{ZXHjeIlwdiCjZoTldkA1KGSjeYOgZpkhVVSWIHHzd4F6NCCrY{WwQVEyKG6P MkPSNlI6QDR7OEe=
human PBMC NIfqPVZRem:uaX\ldoF1cW:wIHHzd4F6 MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCETVOsJGlEPTB;MUKgcm0> Mn\ZNVU3Pzl|MEm=
human MDA435/LCC6MDR cells MnfSSpVv[3Srb36gZZN{[Xl? NVP2OYVCPSCmYYnz M1:5NG1w\HWuYYTpc44hd2ZiUD3ndEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIHj1cYFvKE2GQUSzOU9NS0N4TVTSJINmdGy|IHHzd4V{e2WmIHHzJJJmfmW{c3nu[{Bx[WOuaYThfIVtKHKnc3nzeIFv[2VibXXhd5Vz\WRiYYOgZ4VtdCC|dYL2bZZidCCjZoTldkA2KGSjeYOgZpkhVVSVIHHzd4F6NCCHQ{WwQVAvODN{IN88UU4> MnvpNlU6QDVzOUW=
HEK293 cells NVTlPVVMTnWwY4Tpc44h[XO|YYm= NHzlb4RKdmirYnn0bY9vKG:oIF;BWHAySjFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGG|c3Xzd4VlKGG|IIDyc5RmcW5vbXXkbYF1\WRicHn0ZZZie3SjdHnuJJVxfGGtZf-8kEBMcT1yLkKg{txO MX:yNlU5Pzl6Nh?=
CK1 cells M4ez[mZ2dmO2aX;uJIF{e2G7 NVL3NWN7SW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUFCYLUOzJIlv\mWldHXkJIlvKEONMTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKH[rcnHsJJJmeGyrY3H0bY9vKGGodHXyJFch\GG7czygWGM2OD1yLkOg{txO MkPPNVgzOTJzMEC=
mouse mammary carcinoma cell line EMT6/AR 1.0 NXzYTIE1TnWwY4Tpc44h[XO|YYm= NG\CWodT\X[ncoPhcEBm\m[nY4Sgc44hfGinIHHjZ5VufWyjdHnvckBw\iCdM1jdMUBl[XWwb4L1ZolkcW5iaX6gcY92e2VibXHtcYFzgSClYYLjbY5wdWFiY3XscEBtcW6nIFXNWFYwSVJiMT6wMEBKSzVyPUCuOFQh|ryP MoHtNVAxQTh4N{G=
KB cell MULGeY5kfGmxbjDhd5NigQ>? NEjYbXpKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhU0JiY3XscEBtcW6nIHHmeIVzKDd{IHigc4Yh\HK3ZzDlfJBwe3W{ZTygTWM2OD1yLk[g{txO MUSxOVQ5OTl7MR?=
mouse L5178 cells NUf0dVdJTnWwY4Tpc44h[XO|YYm= NELLWmczOCCvaX7z NHfReGlKdmirYnn0bY9vKG:oIHj1cYFvKEGEQ1KxMY1m\GmjdHXkJJJpd2SjbXnu[UAyOjNiZX\mcJV5KGmwIH3veZNmKEx3MUe4JINmdGy|IHX4dJJme3OrbnegbJVu[W5iTVTSNUBi\nSncjCyNEBucW6|IHL5JGZCS1NiYX7hcJl{cXNuIFnDOVA:OC54NTFOwG0> MXGyNVM1OTd2NR?=
LLC-PK1 epithelial cells NFjjUmpHfW6ldHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKFBvZ3z5Z49xem:2ZXnuMEBud3W|ZTDMMY1lejGkIHX4dJJme3OnZDDpckBNVENvUFuxJIVxcXSqZXzpZYwh[2WubIOgeZNqdmdiY3HsZ4Vqdi2DTTDwc4xiemm|YYTpc44h[XO|YYpvwKwhUUN3ME2wMlch|ryP MoLGNVI3QTl|OEm=
human K562/R7 cells NXPvT2duTnWwY4Tpc44h[XO|YYm= MWOxJO69VQ>? NEO3SXc4OiCq MXvQc5RmdnSrYYTpc44hd2ZiZH;4c5J2[mmlaX6tbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBld3ixcoXibYNqdi2{ZYPpd5RidnRiaIXtZY4hUzV4Mj;SO{Bk\WyuczDhd5Nme3OnZDDhd{Bld3ixcoXibYNqdiCLQ{WwJIF1KDFidV2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkeg{txO M2i1UlI2PjN2MESx
A2780/ADR cells NH7V[W9HfW6ldHnvckBie3OjeR?= MnrETY5pcWKrdHnvckBw\iCSLXfsfYNweHKxdHXpckBmgHC{ZYPz[YQhcW5iQUK3PFAwSUSUIHPlcIx{KGK7IHPhcINmcW5iQV2gZZN{[XoxvJygTWM2OD1zLkSxNlU1KM7:TR?= MUmxO|g6ODB7NB?=
KB/MDR cell M{TxVGZ2dmO2aX;uJIF{e2G7 MWe3NkBp NXrxO5MyUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEuEL13EVkBk\WyuIHzpcoUh[W[2ZYKgO|IhcHJib3[g[JJ2\yCneIDvd5Vz\SxiSVO1NF0yNjVizszN Ml3uNVU1QDF7OUG=
guinea pig ventricular myocytes MkT5SpVv[3Srb36gZZN{[Xl? M1jGPWlvcGmkaYTpc44hd2ZiTD30fZBmKGOjbHPpeY0h[2ijbn7lcEBu\WG|dYLl[EB2e2mwZzD3bI9t\S2lZXzsJJBifGOqIHPsZY1xKGmwIHf1bY5m[SCyaXegeoVvfHKrY4XsZZIhdXmxY4n0[ZMtKEmFNUC9NkDPxE1? NELUPFIzOjd4MUCwNC=>
human MDA435/LCC6MDR cells Mly5R5l1d3SxeHnjxsBie3OjeR?= MYC3Nog> NV\wUIFqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDNEO1M2xESz[PRGKgZ4VtdHNiZYjwdoV{e2mwZzDNSHIh[W[2ZYKgO|IhcHK|78{MJGlEPTB;Mj64JO69VQ>? NWDFeod4OjJ|MkC0NFI>
human Caco2 cells M37iNGZ2dmO2aX;uJIF{e2G7 Ml3Ocohq[mm2aX;uJI9nKFBvZ4CgbY4hcHWvYX6gR4FkdzJiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJIRq\2:6aX6g[YZndHW6LDDJR|UxRTJwOTFOwG0> NGjxWWEzOzN6MkS1PC=>
leukemia CEM cells MUXGeY5kfGmxbjDhd5NigQ>? Mm\UTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGh2dWGwIF3EVlEhWC2JbInjc5Bzd3SnaX6gRWJEKFS{YX7zdI9zfGW{IIXzbY5oKGyndXvlcYliKEOHTTDj[YxteyxiSVO1NF0{NjRizszN M4DPU|EzOzZzM{i3
human HeLa cells NEDmU3VHfW6ldHnvckBie3OjeR?= NUjq[WxWSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhUFCYLUG4JIlv\mWldHXkJIlvKGi3bXHuJGhmVGFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjC3JIRigXQxvJygWGM2OD12Lk[g{txO NYDCVY5XOTh{MUKxNFA>
human 2008 cells MmLqSpVv[3Srb36gZZN{[Xl? M3HIXGlvcGmkaYTpc44hd2ZiaIXtZY4hVVKSMTDpckBpfW2jbjCyNFA5KGOnbHzzMEBKSzVyPUSuO|gh|ryP MmnkNVg4ODd6OES=
human HuH7 cells NXn4NpdrS3m2b4TvfIlkyqCjc4PhfS=> MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIeWg4KGOnbHzzJIF{e2W|c3XkJIF{KHKnbHXhd4Uhd2ZibHHjeIF1\SCmZXj5[JJw\2WwYYPlMEBKSzVyPUWuPFEh|ryP NFHIepYzODl2M{O5NC=>
human Huh5-2 cells NX;IcGJzS3m2b4TvfIlkyqCjc4PhfS=> M3zzUVMh\GG7cx?= MoDkR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTJVpPS1{IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZkhNCCFQ{WwQVYh|ryP NFS4SYYyQDZ{NUe2Oi=>
human HuH6 cells NULTT|AzS3m2b4TvfIlkyqCjc4PhfS=> NFLZfYs{KGSjeYO= M1LjXmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGh2UDZiY3XscJMh[W[2ZYKgN{Bl[Xm|IHL5JG1VXCCjc4PhfUwhS0N3ME23JO69VQ>? MlPXNVg3OjV5Nk[=
human Huh-9-13 cells MYXDfZRwfG:6aXRCpIF{e2G7 NIH4cJk{KGSjeYO= NVXmZ4Q1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUHWqLUmtNVMh[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3Ojef-8kEBESzVyPUeg{txO MojXNVg3OjV5Nk[=
african green monkey Vero cells NECySYZHfW6ldHnvckBie3OjeR?= NEfZcpUzPCCq NYrOVGdxSW62aY\pdoFtKGGldHn2bZR6KGGpYXnud5QhX2W|dDDObYxmKH[rcoXzJIlv\mWldHXkJIlvKGGocnnjZY4h\3KnZX6gcY9vc2W7IG\ldo8h[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5idnnyZYwhWk6DIIP5cpRp\XOrczDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUig{txO NGTYN4MyQTR3MUK4Oi=>
human HeLa cells NHn5NZZEgXSxdH;4bYPDqGG|c3H5 MkjER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTIVN[SClZXzsd{whXEN3ME24MlMh|ryP MV2xPFIyOjFyMB?=
human LCC-6 cells Mm[3R5l1d3SxeHnjxsBie3OjeR?= MmLTO|IhcA>? NUTqV204S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVEOFLU[gZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUiuN{DPxE1? MnPvNlI{OjB2MEK=
MDCK cells M4fJWmN6fG:2b4jpZ:Kh[XO|YYm= MV\DfZRwfG:6aXPpeJkh[WejaX7zeEBOTEONIHPlcIx{NCCWQ{WwQVkvQSEQvF2= MUOxPFIyOjFyMB?=
human Huh-Mono cells MYPDfZRwfG:6aXRCpIF{e2G7 NVL4elZJOyCmYYnz M3\XU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGh2cC2Pb37vJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGSgZZN{[XoxvJygR2M2OD1{NDFOwG0> MWSxPFYzPTd4Nh?=
mouse L929 cells M2j1fmN6fG:2b4jpZ:Kh[XO|YYm= M{HSc|Mh\GG7cx?= MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDMPVI6KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;M{Cg{txO MUCyOVk5PTF7NR?=
rat H42E cells NGO2d5lEgXSxdH;4bYPDqGG|c3H5 NW[0VVV7S3m2b4TvfIlkcXS7IHHnZYlve3RicnH0JGg1OkViY3XscJMh[XO|ZYPz[YQh[XNiaX70doFk\WyudXzhdkBCXFBibHX2[YwtKFSFNUC9OFIh|ryP MYKxPVUxOjB3OB?=

... Click to View More Cell Line Experimental Data

In vivo Cyclosporin A is an immunosuppressive agent that is effective following either parenteral or oral administration in mice, rat and guinea pigs. [6], is clinically used in organ transplantation to prevent rejection. [7]

Protocol

Kinase Assay:[3]
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Phosphatase Assay:

Purified bovine brain calcineurin and calmodulin are purchased. Reaction mixtures with purified enzyme contains 100 nM calcineurin, 100 nM calmodulin, and 5 μM 32P-labeled phosphopeptide, in 60 μl (total volume) of assay buffer containing 20 mM Tris (pH 8), 100 mM NaCI, 6 mM MgCl2, 0.5 mM dithiothreitol, 0.1 mg of bovine serum albumin per ml, and either 0.1 mM CaCl2 or 5 mM EGTA. Reaction mixtures with cell lysates contains 20 μl of undiluted lysate, 5 μM 32P-labeled phosphopeptide, and 40 μl of assay buffer. Where indicated, reaction mixtures contains 50 μM peptide 412 or 413 and/or 500 nM okadaic acid, a specific inhibitor of phosphatases 1 and 2A; 500 nM okadaic acid is sufficient for inhibition of Ca2+-independent phosphatases, whereas higher concentrations partially inhibit Ca2+-dependent activity as well. After 15 min at 30°C, reactions are terminated by the addition of 0.5 ml of 100 mM potassium phosphate buffer (pH 7.0) containing 5% trichloroacetic acid. Free inorganic phosphate is isolated by Dowex cation-exchange chromatography and quantitated by scintillation counting as described.
Cell Research:[3]
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  • Cell lines: Jurkat cells (clone J77)
  • Concentrations: ~100 nM
  • Incubation Time: 1 hr
  • Method: Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (106) are suspended in 1 ml of complete medium in microcentrifuge tubes; 1 μl of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 ml of PBS on ice and lysed in 50μl of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of aprotinin per ml. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g.
    (Only for Reference)
Animal Research:[6]
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  • Animal Models: Rat
  • Dosages: 45 mg/kg
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (83.15 mM)
Water Insoluble
Ethanol '''100 mg/mL warmed
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1202.61
Formula

C62H111N11O12

CAS No. 59865-13-3
Storage powder
in solvent
Synonyms Cyclosporine A
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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04023760 Recruiting Drug: Apixaban Pharmacokinetics|Kidney Transplant|Lung Transplant University of Saskatchewan|Saskatchewan Health Research Foundation|Lung Association of Saskatchewan June 26 2019 Phase 4
NCT03865888 Completed Drug: Cyclosporins|Drug: Tacrolimus Dry Eye|Sjogren Syndrome Pavly Moawd|Cairo University October 30 2018 Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    What is the difference between S2286 (cyclosporin A) and S1514 (cyclosporin)?

  • Answer:

    Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. Cyclosporine A is an especially useful Cyclosporine component.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID