Cyclosporin A

For research use only. Not for use in humans.

Catalog No.S2286 Synonyms: Cyclosporine A

25 publications

Cyclosporin A  Chemical Structure

Molecular Weight(MW): 1202.61

Cyclosporin 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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10mM (1mL in DMSO) USD 130 In stock
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Selleck's Cyclosporin A has been cited by 25 publications

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Biological Activity

Description Cyclosporin 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 NHHKTWJHfW6ldHnvckBie3OjeR?= NX2yZ3NkUW6qaXLpeIlwdiCxZjDsbZZmeiC|dHHn[UBRdGG|bX;kbZVuKGKncnfo[YkhcW6oZXP0bY9vKGmwIFjldGczKGOnbHzzMEBKSzVyPUGuOlUhdk1? MkLMNlI2QDZzMkS=
Jurkat cells MkLCSpVv[3Srb36gZZN{[Xl? NGD4cndKdW23bn;zeZBxemW|c3n2[UBi[3Srdnn0fUB4[XNibXXhd5Vz\WRiYomgbY5pcWKrdHnvckBw\iC2aHWgTWwuOiCycn;keYN1cW:wIHnuJGp2emujdDDj[YxteyxiSVO1NF0zKG6P M2LIS|E1PjR|M{O3
human PBMC NH71dXRHfW6ldHnvckBie3OjeR?= NWnOVXVOOSCq NFvDeWRCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKGi3bXHuJHBDVUNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjboTpMWNFOy:FREK4JIFvfGmkb3T5MYlv\HWlZXSgTWwuOiCycn;keYN1cW:wIITy[YF1\WRiZn;yJFEhcHJiYnXmc5JmKGGwdHmtR2Q{N0OGMkigZY51cWKxZImgZ4hidGynbnflJI1m[XO3cnXkJIFnfGW{IE[gbJJ{KGK7IHntcZVvd3O3cIDy[ZN{cW:wIHHzd4F6NCCHQ{WwQVMvOSCwTR?= NYLSTGNTOTl7M{O3PVU>
human Jurkat cells MWDGeY5kfGmxbjDhd5NigQ>? NFLE[XAyKGh? NVzGNGJPSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCqdX3hckBLfXKtYYSgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjboTpMWNFOy:FREK4JIFvfGmkb3T5MYlv\HWlZXSgTWwuOiCycn;keYN1cW:wIITy[YF1\WRiZn;yJFEhcHJiYnXmc5JmKGGwdHmtR2Q{N0OGMkigZY51cWKxZImgZ4hidGynbnflJI1m[XO3cnXkJIFnfGW{IE[gbJJ{KGK7IHntcZVvd3O3cIDy[ZN{cW:wIHHzd4F6NCCHQ{WwQVUhdk1? M2XZelE6QTN|N{m1
human T-cell Mlr1SpVv[3Srb36gZZN{[Xl? MVrJckB3cXS{bzDpcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVD3j[YxtKHC{b3T1Z5Rqd25ib3[gcJlueGixa3nu[UBKVC1{LDDJR|UxRThwMTDuUS=> Mke2O|U{PzN|MR?=
human splenocytes NGXaV5pHfW6ldHnvckBie3OjeR?= NIC1NoE1KGSjeYO= MXPJcY12dm:|dYDwdoV{e2m4ZTDhZ5Rqfmm2eTDpckBpfW2jbjDzdIxmdm:leYTld{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHs{UF22aIntbYRqdmViaX7jc5Jxd3KjdHnvckBi\nSncjC0JIRigXNiYomgZYxtd2enbnnjJI1qgGWmIHz5cZBpd2O7dHWgdoVi[3Srb36gZZN{[XluIFnDOVA:OTBibl2= MVmxPVgzPzh|MR?=
mouse T cells M{nGWGZ2dmO2aX;uJIF{e2G7 NIOzSVE1KGSjeYO= NVy1R3l2UW2vdX7vd5VxeHKnc4PpeoUh[WO2aY\peJkhcW5ibX;1d4UhXCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJR4dyC5YYmgcYl5\WRibIntdIhw[3m2ZTDy[YFkfGmxbjDh[pRmeiB2IHThfZMh[nliTWTUJIF{e2G7LDDpZ|UxRTFzIH7N MoPFNlI6QDR7OEe=
human PBMC MYTQdo9tcW[ncnH0bY9vKGG|c3H5 NVfzc3ZpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQRm1ENCCLQ{WwQVEzKG6P NGi2S5QyPTZ5OUOwPS=>
human MDA435/LCC6MDR cells NEf5RWVHfW6ldHnvckBie3OjeR?= M4jjPFUh\GG7cx?= MWTNc4R2dGG2aX;uJI9nKFBvZ4CgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCqdX3hckBOTEF2M{WvUGNEPk2GUjDj[YxteyCjc4Pld5Nm\CCjczDy[ZZmenOrbnegdIFkdGm2YYjlcEBz\XOrc4ThcoNmKG2nYYP1doVlKGG|IHPlcIwhe3W{dnn2ZYwh[W[2ZYKgOUBl[Xm|IHL5JG1VWyCjc4PhfUwhTUN3ME2wMlA{OiEQvF2u NWfmU49LOjV7OEWxPVU>
HEK293 cells MWXGeY5kfGmxbjDhd5NigQ>? NFPLZldKdmirYnn0bY9vKG:oIF;BWHAySjFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGG|c3Xzd4VlKGG|IIDyc5RmcW5vbXXkbYF1\WRicHn0ZZZie3SjdHnuJJVxfGGtZf-8kEBMcT1yLkKg{txO NXTmV2xkOjJ3OEe5PFY>
CK1 cells NFL3c2lHfW6ldHnvckBie3OjeR?= NH7UNJJCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBJWFZvM{OgbY5n\WO2ZXSgbY4hS0tzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yhfmm{YXygdoVxdGmlYYTpc44h[W[2ZYKgO{Bl[Xm|LDDUR|UxRTBwMzFOwG0> MWSxPFIyOjFyMB?=
mouse mammary carcinoma cell line EMT6/AR 1.0 Mof3SpVv[3Srb36gZZN{[Xl? MoHXVoV3\XK|YXyg[YZn\WO2IH;uJJRp\SCjY3P1cZVt[XSrb36gc4YhYzOKXT2g[IF2dm:{dXLpZ4lvKGmwIH3veZNmKG2jbX3hdpkh[2G{Y3nuc41iKGOnbHygcIlv\SCHTWS2M2FTKDFwMDygTWM2OD1yLkS0JO69VQ>? NGfmUFMyODB7OE[3NS=>
KB cell NI[yVI9HfW6ldHnvckBie3OjeR?= Ml;GTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGtDKGOnbHygcIlv\SCjZoTldkA4OiCqIH;mJIRzfWdiZYjwc5N2emVuIFnDOVA:OC54IN88US=> M1HRNlE2PDhzOUmx
mouse L5178 cells NYPyUJdyTnWwY4Tpc44h[XO|YYm= NX\UVndsOjBibXnudy=> M{ftV2lvcGmkaYTpc44hd2ZiaIXtZY4hSUKFQkGtcYVlcWG2ZXSgdohw\GGvaX7lJFEzOyCnZn\seZghcW5ibX;1d4UhVDVzN{igZ4VtdHNiZYjwdoV{e2mwZzDoeY1idiCPRGKxJIFnfGW{IEKwJI1qdnNiYomgSmFEWyCjbnHsfZNqeyxiSVO1NF0xNjZ3IN88US=> MY[yNVM1OTd2NR?=
LLC-PK1 epithelial cells NIHsWXdHfW6ldHnvckBie3OjeR?= MXjJcohq[mm2aX;uJI9nKFBvZ3z5Z49xem:2ZXnuMEBud3W|ZTDMMY1lejGkIHX4dJJme3OnZDDpckBNVENvUFuxJIVxcXSqZXzpZYwh[2WubIOgeZNqdmdiY3HsZ4Vqdi2DTTDwc4xiemm|YYTpc44h[XO|YYpvwKwhUUN3ME2wMlch|ryP NVu2c3lROTJ4OUmzPFk>
human K562/R7 cells M3\obGZ2dmO2aX;uJIF{e2G7 MYmxJO69VQ>? MoezO|IhcA>? M2nyfHBwfGWwdHnheIlwdiCxZjDkc5hwenWkaXPpck1qdmS3Y3XkJIN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGSxeH;yeYJq[2mwLYLld4l{fGGwdDDoeY1idiCNNU[yM3I4KGOnbHzzJIF{e2W|c3XkJIF{KGSxeH;yeYJq[2mwIFnDOVAh[XRiMTD1UUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuO{DPxE1? NHziVoMzPTZ|NEC0NS=>
A2780/ADR cells NIjpNIJHfW6ldHnvckBie3OjeR?= NF;ieXJKdmirYnn0bY9vKG:oIGCt[4x6[2:ycn;0[YlvKGW6cILld5Nm\CCrbjDBNlc5OC:DRGKgZ4VtdHNiYomgZ4Ft[2WrbjDBUUBie3Ojef-8kEBKSzVyPUGuOFEzPTRizszN MlzRNVc5QTByOUS=
KB/MDR cell NFnrO2JHfW6ldHnvckBie3OjeR?= M3W3NFczKGh? Mo\NTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGtDN02GUjDj[YxtKGyrbnWgZYZ1\XJiN{KgbJIhd2ZiZIL1[{BmgHCxc4Xy[UwhUUN3ME2xMlUh|ryP MUexOVQ5OTl7MR?=
guinea pig ventricular myocytes MmPJSpVv[3Srb36gZZN{[Xl? NWDBd3hlUW6qaXLpeIlwdiCxZjDMMZR6eGViY3HsZ4l2dSClaHHucoVtKG2nYYP1doVlKHW|aX7nJJdpd2ynLXPlcIwheGG2Y3igZ4xidXBiaX6g[5VqdmWjIIDp[{B3\W62cnnjeYxieiCveX;jfZRmeyxiSVO1NF0zKM7:TR?= NEf0W4YzOjd4MUCwNC=>
human MDA435/LCC6MDR cells NFziNm5EgXSxdH;4bYPDqGG|c3H5 NGH3fJE4Omh? MnL3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCPDN3L1zDR|ZOTFJiY3XscJMh\XiycnXzd4lv\yCPRGKgZYZ1\XJiN{KgbJJ{97zOIFnDOVA:Oi56IN88US=> NFmxV4EzOjN{MESwNi=>
human Caco2 cells MYXGeY5kfGmxbjDhd5NigQ>? MXTubIljcXSrb36gc4YhWC2pcDDpckBpfW2jbjDDZYNwOiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6g[Ilod3irbjDl[oZtfXhuIFnDOVA:Oi57IN88US=> Ml[2NlM{QDJ2NUi=
leukemia CEM cells M3O3U2Z2dmO2aX;uJIF{e2G7 MnvxTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGh2dWGwIF3EVlEhWC2JbInjc5Bzd3SnaX6gRWJEKFS{YX7zdI9zfGW{IIXzbY5oKGyndXvlcYliKEOHTTDj[YxteyxiSVO1NF0{NjRizszN MUOxNlM3OTN6Nx?=
human HeLa cells NHL1dodHfW6ldHnvckBie3OjeR?= M1TVZmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhRXi1zODDpcoZm[3SnZDDpckBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geolz[WxicnXwcIlk[XSrb36gZYZ1\XJiNzDkZZl{97zOIGTDOVA:PC54IN88US=> NHHP[pcyQDJzMkGwNC=>
human 2008 cells NUXDOWMzTnWwY4Tpc44h[XO|YYm= NFXMTldKdmirYnn0bY9vKG:oIHj1cYFvKE2UUEGgbY4hcHWvYX6gNlAxQCClZXzsd{whUUN3ME20Mlc5KM7:TR?= M3\TR|E5PzB5OEi0
human HuH7 cells NUf4cpN7S3m2b4TvfIlkyqCjc4PhfS=> Mm\3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTJVJPyClZXzsd{Bie3Onc4Pl[EBieyC{ZXzlZZNmKG:oIHzhZ5RifGViZHXofYRzd2enbnHz[UwhUUN3ME21MlgyKM7:TR?= MVmyNFk1OzN7MB?=
human Huh5-2 cells MULDfZRwfG:6aXRCpIF{e2G7 NXjmZpdtOyCmYYnz M1\MemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGh2cDVvMjDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6KCxiQ1O1NF03KM7:TR?= MU[xPFYzPTd4Nh?=
human HuH6 cells NFHqeW1EgXSxdH;4bYPDqGG|c3H5 MXezJIRigXN? MlvVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTJVJPiClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRVKGG|c3H5MEBESzVyPUeg{txO NUDNT5VNOTh4MkW3OlY>
human Huh-9-13 cells NWDQeYg2S3m2b4TvfIlkyqCjc4PhfS=> MoDBN{Bl[Xm| MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIeYguQS1zMzDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F697zOIFPDOVA:PyEQvF2= NIjU[3MyQDZ{NUe2Oi=>
african green monkey Vero cells MVvGeY5kfGmxbjDhd5NigQ>? NGHNRYszPCCq M3G4S2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JHdme3RiTnns[UB3cXK3czDpcoZm[3SnZDDpckBi\nKrY3HuJIdz\WWwIH3vcotmgSCYZYLvJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKH[rcnHsJHJPSSC|eX70bIV{cXNiYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD16IN88US=> NVLE[mpNOTl2NUGyPFY>
human HeLa cells NGD6PHlEgXSxdH;4bYPDqGG|c3H5 NXXhfYlYS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyxiVFO1NF05NjNizszN NGTOdGkyQDJzMkGwNC=>
human LCC-6 cells MU\DfZRwfG:6aXRCpIF{e2G7 MXO3NkBp M1i2[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxESy14IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD16LkOg{txO MmrFNlI{OjB2MEK=
MDCK cells MlXFR5l1d3SxeHnjxsBie3OjeR?= M{LndGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KE2GQ1ugZ4VtdHNuIGTDOVA:QS57IN88US=> M3n3Z|E5OjF{MUCw
human Huh-Mono cells M{PX[mN6fG:2b4jpZ:Kh[XO|YYm= NYTtVIFnOyCmYYnz NYrNVVBKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUHWqLV3vco8h[2WubIOgZYZ1\XJiMzDkZZl{KGK7IF3UWEBie3Ojef-8kEBESzVyPUK0JO69VQ>? NYm0WpFrOTh4MkW3OlY>
mouse L929 cells NFmxe|NEgXSxdH;4bYPDqGG|c3H5 MUmzJIRigXN? NG\kWIJEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBNQTJ7IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFNiYYPzZZktKEmFNUC9N|Ah|ryP M1zhTlI2QTh3MUm1
rat H42E cells NW[0[np5S3m2b4TvfIlkyqCjc4PhfS=> NGjYUmdEgXSxdH;4bYNqfHliYXfhbY5{fCC{YYSgTFQzTSClZXzsd{Bie3Onc4Pl[EBieyCrboTyZYNmdGy3bHHyJGFVWCCuZY\lcEwhXEN3ME20NkDPxE1? NW\HeXFHOTl3MEKwOVg>

... 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
  • Formulation: 0.5% solution of tragacanth
  • Dosages: 45 mg/kg
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (83.15 mM)
Ethanol 100 mg/mL warmed (83.15 mM)
Water Insoluble
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 CCC1NC(=O)C(C(O)C(C)C\C=C\C)N(C)C(=O)C(C(C)C)N(C)C(=O)C(CC(C)C)N(C)C(=O)C(CC(C)C)N(C)C(=O)C(C)NC(=O)C(C)NC(=O)C(CC(C)C)N(C)C(=O)C(NC(=O)C(CC(C)C)N(C)C(=O)CN(C)C1=O)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
NCT01762657 Withdrawn Drug: Oral Cyclosporine and Oral Lansoprazole|Drug: Placebos Type 1 Diabetes Perle Bioscience Inc. September 2014 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.

Tags: buy Cyclosporin A | Cyclosporin A supplier | purchase Cyclosporin A | Cyclosporin A cost | Cyclosporin A manufacturer | order Cyclosporin A | Cyclosporin A distributor
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID