Cyclosporin A (NSC 290193)

Catalog No.S2286 Synonyms: Cyclosporine A, Cyclosporine, Ciclosporin, CsA

For research use only.

Cyclosporin A (Cyclosporine A, Cyclosporine, Ciclosporin, CsA) 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.

Cyclosporin A (NSC 290193) Chemical Structure

CAS No. 59865-13-3

Selleck's Cyclosporin A (NSC 290193) has been cited by 58 publications

Purity & Quality Control

Choose Selective Antineoplastic and Immunosuppressive Antibiotics Inhibitors

Biological Activity

Description Cyclosporin A (Cyclosporine A, Cyclosporine, Ciclosporin, CsA) 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
rat H42E cells MljkR5l1d3SxeHnjxsBie3OjeR?= M2rMdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KHKjdDDIOFJGKGOnbHzzJIF{e2W|c3XkJIF{KGmwdILhZ4VtdHWuYYKgRXRRKGyndnXsMEBVSzVyPUSyJO69VQ>? M3nlTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7NUCyNFU5Lz5zOUWwNlA2QDxxYU6=
mouse L929 cells MXvDfZRwfG:6aXRCpIF{e2G7 NFvjdIw{KGSjeYO= MorKR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgUFkzQSClZXzsd{Bi\nSncjCzJIRigXNiYomgUXRUKGG|c3H5MEBKSzVyPUOwJO69VQ>? MmCxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7OEWxPVUoRjJ3OUi1NVk2RC:jPh?=
human Huh-Mono cells M4jsTmN6fG:2b4jpZ:Kh[XO|YYm= Ml\MN{Bl[Xm| MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIeYguVW:wbzDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F697zOIFPDOVA:OjRizszN M1HUNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkK1O|Y3Lz5zOE[yOVc3PjxxYU6=
MDCK cells M4T5N2N6fG:2b4jpZ:Kh[XO|YYm= MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBOTEONIHPlcIx{NCCWQ{WwQVkvQSEQvF2= M1vrPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MkGyNVAxLz5zOEKxNlExODxxYU6=
human LCC-6 cells NXHkW2RDS3m2b4TvfIlkyqCjc4PhfS=> Mn3zO|IhcA>? MnPwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUGNENTZiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRThwMzFOwG0> M3rscVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{KwOFAzLz5{MkOyNFQxOjxxYU6=
human HeLa cells NEHiOHdEgXSxdH;4bYPDqGG|c3H5 NV\sXlRGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyxiVFO1NF05NjNizszN NGHGUJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEKxNlExOCd-MUiyNVIyODB:L3G+
african green monkey Vero cells MkDqSpVv[3Srb36gZZN{[Xl? NXrUWWxwOjRiaB?= NH;SUndCdnSrdnnyZYwh[WO2aY\peJkh[WejaX7zeEBY\XO2IF7pcIUhfmm{dYOgbY5n\WO2ZXSgbY4h[W[{aXPhckBoemWnbjDtc45s\XliVnXyc{Bk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC4aYLhcEBTVkFic4nueIhme2m|IHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;ODFOwG0> NVzTUJoyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm0OVEzQDZpPkG5OFUyOjh4PD;hQi=>
human Huh-9-13 cells MmLSR5l1d3SxeHnjxsBie3OjeR?= M{TXflMh\GG7cx?= NF3lNnpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfWhvOT2xN{Bk\WyuczDh[pRmeiB|IHThfZMh[nliTWTUJIF{e2G778{MJGNEPTB;NzFOwG0> M1GyWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkK1O|Y3Lz5zOE[yOVc3PjxxYU6=
human HuH6 cells M2e4emN6fG:2b4jpZ:Kh[XO|YYm= NGnhS4I{KGSjeYO= MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIeWg3KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHQh[XO|YYmsJGNEPTB;NzFOwG0> NH7jfXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[yOVc3Pid-MUi2NlU4PjZ:L3G+
human Huh5-2 cells NFLHUlREgXSxdH;4bYPDqGG|c3H5 MWKzJIRigXN? M3\YZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGh2cDVvMjDj[YxteyCjZoTldkA{KGSjeYOgZpkhVVSWIHHzd4F6KCxiQ1O1NF03KM7:TR?= M3PhdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkK1O|Y3Lz5zOE[yOVc3PjxxYU6=
human HuH7 cells MnT6R5l1d3SxeHnjxsBie3OjeR?= NYHEbm9DS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUHWKNzDj[YxteyCjc4Pld5Nm\CCjczDy[Yxm[XOnIH;mJIxi[3SjdHWg[IVpgWS{b3flcoF{\SxiSVO1NF02NjhzIN88US=> MkHJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB7NEOzPVAoRjJyOUSzN|kxRC:jPh?=
human 2008 cells MmHxSpVv[3Srb36gZZN{[Xl? MoPTTY5pcWKrdHnvckBw\iCqdX3hckBOWlBzIHnuJIh2dWGwIEKwNFgh[2WubIOsJGlEPTB;ND63PEDPxE1? NWWw[XdQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3NFc5QDRpPkG4O|A4QDh2PD;hQi=>
human HeLa cells NYewNIY5TnWwY4Tpc44h[XO|YYm= M{jiSGFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhRXi1zODDpcoZm[3SnZDDpckBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geolz[WxicnXwcIlk[XSrb36gZYZ1\XJiNzDkZZl{97zOIGTDOVA:PC54IN88US=> M2S1bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MkGyNVAxLz5zOEKxNlExODxxYU6=
leukemia CEM cells NYG3cZVtTnWwY4Tpc44h[XO|YYm= NGXT[pRKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUHWvYX6gUWRTOSCSLVfsfYNweHKxdHXpckBCSkNiVILhcpNxd3K2ZYKgeZNqdmdibHX1b4VucWFiQ1XNJINmdGy|LDDJR|UxRTNwNDFOwG0> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjN4MUO4O{c,OTJ|NkGzPFc9N2F-
human Caco2 cells MmPCSpVv[3Srb36gZZN{[Xl? NXHh[2RrdmirYnn0bY9vKG:oIGCt[5AhcW5iaIXtZY4hS2Glb{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGSrZ3;4bY4h\W[obIX4MEBKSzVyPUKuPUDPxE1? M4TOU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{iyOFU5Lz5{M{O4NlQ2QDxxYU6=
human MDA435/LCC6MDR cells NHrITJREgXSxdH;4bYPDqGG|c3H5 NFPaUZM4Omh? MlLMR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCPDN3L1zDR|ZOTFJiY3XscJMh\XiycnXzd4lv\yCPRGKgZYZ1\XJiN{KgbJJ{97zOIFnDOVA:Oi56IN88US=> M2HlclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{KwOFAzLz5{MkOyNFQxOjxxYU6=
guinea pig ventricular myocytes MoqwSpVv[3Srb36gZZN{[Xl? NHLRdWdKdmirYnn0bY9vKG:oIFyteJlx\SClYXzjbZVuKGOqYX7u[YwhdWWjc4Xy[YQhfXOrbnege4hwdGVvY3XscEBx[XSlaDDjcIFueCCrbjDneYlv\WFicHnnJJZmdnS{aXP1cIFzKG27b3P5eIV{NCCLQ{WwQVIh|ryP NX3PfIxZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK3OlExODBpPkKyO|YyODByPD;hQi=>
KB/MDR cell MXfGeY5kfGmxbjDhd5NigQ>? NG\T[Ww4OiCq NHfw[JhKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhU0JxTVTSJINmdGxibHnu[UBi\nSncjC3NkBpeiCxZjDkdpVoKGW6cH;zeZJmNCCLQ{WwQVEvPSEQvF2= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTR6MUm5NUc,OTV2OEG5PVE9N2F-
A2780/ADR cells Mn;1SpVv[3Srb36gZZN{[Xl? NVvIeHhNUW6qaXLpeIlwdiCxZjDQMYdtgWOxcILveIVqdiCneIDy[ZN{\WRiaX6gRVI4QDBxQVTSJINmdGy|IHL5JINidGOnaX6gRW0h[XO|YYpvwKwhUUN3ME2xMlQyOjV2IN88US=> NHrBTWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{i5NFA6PCd-MUe4PVAxQTR:L3G+
human K562/R7 cells MWXGeY5kfGmxbjDhd5NigQ>? M3;nT|Eh|ryP M{ToTlczKGh? NUTSe3RpWG:2ZX70bYF1cW:wIH;mJIRwgG:{dXLpZ4lvNWmwZIXj[YQh[3m2b4TvfIlkcXS7IHHnZYlve3RiZH;4c5J2[mmlaX6tdoV{cXO2YX70JIh2dWGwIFu1OlIwWjdiY3XscJMh[XO|ZYPz[YQh[XNiZH;4c5J2[mmlaX6gTWM2OCCjdDCxJJVOKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE44KM7:TR?= MmLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4M{SwOFEoRjJ3NkO0NFQyRC:jPh?=
LLC-PK1 epithelial cells NH;sXHNHfW6ldHnvckBie3OjeR?= MYnJcohq[mm2aX;uJI9nKFBvZ3z5Z49xem:2ZXnuMEBud3W|ZTDMMY1lejGkIHX4dJJme3OnZDDpckBNVENvUFuxJIVxcXSqZXzpZYwh[2WubIOgeZNqdmdiY3HsZ4Vqdi2DTTDwc4xiemm|YYTpc44h[XO|YYpvwKwhUUN3ME2wMlch|ryP MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yOjZ7OUO4PUc,OTJ4OUmzPFk9N2F-
mouse L5178 cells M2jrb2Z2dmO2aX;uJIF{e2G7 NH7EZmszOCCvaX7z MnXNTY5pcWKrdHnvckBw\iCqdX3hckBCSkOEMT3t[YRq[XSnZDDybI9l[W2rbnWgNVI{KGWoZnz1fEBqdiCvb4Xz[UBNPTF5ODDj[YxteyCneIDy[ZN{cW6pIHj1cYFvKE2GUkGgZYZ1\XJiMkCgcYlveyCkeTDGRWNUKGGwYXz5d4l{NCCLQ{WwQVAvPjVizszN MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN2MUe0OUc,OjF|NEG3OFU9N2F-
KB cell MXvGeY5kfGmxbjDhd5NigQ>? NHXjfoJKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhU0JiY3XscEBtcW6nIHHmeIVzKDd{IHigc4Yh\HK3ZzDlfJBwe3W{ZTygTWM2OD1yLk[g{txO MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTR6MUm5NUc,OTV2OEG5PVE9N2F-
mouse mammary carcinoma cell line EMT6/AR 1.0 M2rMXWZ2dmO2aX;uJIF{e2G7 MVvS[ZZmenOjbDDl[oZm[3Rib36geIhmKGGlY4XteYxifGmxbjDv[kBcO0ifLTDkZZVvd3K3YnnjbY4hcW5ibX;1d4UhdWGvbXHyfUBk[XKlaX7vcYEh[2WubDDsbY5mKEWPVE[vRXIhOS5yLDDJR|UxRTBwNESg{txO M{no[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyMEm4OlcyLz5zMEC5PFY4OTxxYU6=
CK1 cells MVTGeY5kfGmxbjDhd5NigQ>? M1PKOmFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGhRXi1|MzDpcoZm[3SnZDDpckBEUzFiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kB3cXKjbDDy[ZBtcWOjdHnvckBi\nSncjC3JIRigXNuIGTDOVA:OC5|IN88US=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDJzMkGwNEc,OTh{MUKxNFA9N2F-
HEK293 cells Mn23SpVv[3Srb36gZZN{[Xl? NYfUd4FTUW6qaXLpeIlwdiCxZjDPRXRROUJzIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjc4Pld5Nm\CCjczDwdo91\WmwLX3l[IlifGWmIIDpeIF3[XO2YYTpckB2eHSja3ZvwKwhU2l;MD6yJO69VQ>? NEDU[5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW4O|k5Pid-MkK1PFc6QDZ:L3G+
human MDA435/LCC6MDR cells NULySmZsTnWwY4Tpc44h[XO|YYm= MXq1JIRigXN? MmfvUY9lfWyjdHnvckBw\iCSLXfwJEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5iaIXtZY4hVUSDNEO1M2xESz[PRGKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoV3\XK|aX7nJJBi[2yrdHH4[YwhemW|aYP0ZY5k\SCvZXHzeZJm\CCjczDj[YxtKHO3co\peoFtKGGodHXyJFUh\GG7czDifUBOXFNiYYPzZZktKEWFNUC9NE4xOzJizszNMi=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl6NUG5OUc,OjV7OEWxPVU9N2F-
human PBMC MUnQdo9tcW[ncnH0bY9vKGG|c3H5 NGn6cG1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDCUWMtKEmFNUC9NVIhdk1? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTZ5OUOwPUc,OTV4N{mzNFk9N2F-
mouse T cells NXzFcFVFTnWwY4Tpc44h[XO|YYm= M3vEdVQh\GG7cx?= NXnBNY1jUW2vdX7vd5VxeHKnc4PpeoUh[WO2aY\peJkhcW5ibX;1d4UhXCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJR4dyC5YYmgcYl5\WRibIntdIhw[3m2ZTDy[YFkfGmxbjDh[pRmeiB2IHThfZMh[nliTWTUJIF{e2G7LDDpZ|UxRTFzIH7N M4rPWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUi0PVg4Lz5{Mkm4OFk5PzxxYU6=
human splenocytes M3XDdmZ2dmO2aX;uJIF{e2G7 M2\rc|Qh\GG7cx?= M3uxPGludXWwb4P1dJBz\XO|aY\lJIFkfGm4aYT5JIlvKGi3bXHuJJNxdGWwb3P5eIV{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhYzOKXYTofY1q\GmwZTDpcoNwenCxcnH0bY9vKGGodHXyJFQh\GG7czDifUBidGyxZ3XubYMhdWm6ZXSgcJlueGixY4n0[UBz\WGldHnvckBie3OjeTygTWM2OD1zMDDuUS=> NE\1W5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUiyO|g{OSd-MUm4Nlc5OzF:L3G+
human T-cell M2TsOmZ2dmO2aX;uJIF{e2G7 NX\WU2VyUW5idnn0do8hcW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJHQu[2WubDDwdo9lfWO2aX;uJI9nKGy7bYDoc4tqdmViSVytNkwhUUN3ME24MlEhdk1? NXvUdIlJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxN{WzO|M{OSd-N{WzO|M{OTxxYU6=
human Jurkat cells NX;4SWNOTnWwY4Tpc44h[XO|YYm= NGLoRnEyKGh? MX7BcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJIh2dWGwIFr1dotifCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIFvfGlvQ1SzM2NFOjhiYX70bYJw\HlvaX7keYNm\CCLTD2yJJBzd2S3Y4Tpc44hfHKnYYTl[EBnd3JiMTDodkBj\W[xcnWgZY51cS2FREOvR2QzQCCjboTpZo9lgSClaHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhPiCqcoOgZpkhcW2vdX7vd5VxeHKnc4Ppc44h[XO|YYmsJGVEPTB;NTDuUS=> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTl|M{e5OUc,OTl7M{O3PVU9N2F-
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Assay
Methods Test Index PMID
Western blot Phospho-AKT1 / AKT1 / PTEN / Phospho-BAD / BAD / Procaspase-3 ; Cyp-D / AIF / β-actin ; IL-8 / MCP-1 ; Actin / Smac ; β-actin / FIPV-N 12644839 29328412 9602633 12427831 22546085
Growth inhibition assay NPC death 20181586
IHC Th22 / Th17 / Th1 / M1 / Th2 ; Tregs / Bregs / pDCs / M2 ; Ki 67 / Fas-FasL ; IFN-γ / TNF-α ; WT-PCLS / FXRKO-PCLS 30916387 10931158 26482353
Immunofluorescence Human gingival fibroblast cells ; Human gingival fibroblast cells ; Calcein ; Rhod-Dex / Calcein ; cadherin-9 / vimentin 27857765 23593196 20584761 17668045
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 (from reference)

Kinase Assay:[3]
  • 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]
  • 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]
  • 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 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg 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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05056779 Not yet recruiting Drug: Nemolizumab|Drug: CD14152 placebo Moderate-to-severe Atopic Dermatitis Galderma R&D January 2022 Phase 3
NCT04989686 Not yet recruiting Other: Microsampling Immunosuppression Children''s Hospital of Philadelphia December 2021 --
NCT04023760 Completed 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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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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