Form
Powder
Appearance
Whitecrystallinepowder
Assay
98.5-101.5%(ondriedbasis)
LossonDrying
≤2.0%
HeavyMetals
≤0.002%
Impurities
RelatedCompounds:
Individualimpurity:≤0.7%
Totalimpurities:≤1.5%
Cyclosporin,USPisamixtureofcyclicoligopeptideimmunosuppressantcompoundsroutinelygiven topatientsafterreceivinganorgantransplanttopreventtransplantrejection.Cyclosporin,USPcontainsmostlycyclosporinA(>98.0%)whichhasthemostpotentimmunosuppressantactivityofthecyclosporinsandishighlymetabolizedbyhumansandanimalsafteringestion.Theresultingmetabolites(cyclosporinB,C,D,E,H,L,andothers)havebeenfoundtohavelesspotentimmunosuppressantactivityandareassociatedwithhighernephrotoxicitywhencomparedtocyclosporinA.
TOKU-EofferspurifiedformsofcyclosporinA,B,C, D,E,H,andL.
59865-13-3
C62H111N11O12
1202.61
CyclosporinA(CsA)immunosuppressantactivitystemsfromitsABIlitytopreventT-cellactivationbyblockingspecificcytokinetranscriptiongenes.AfterenteringaT-cell,cyclosporinA(CsA)associateswithubiquitouscytosolicproteinscalledcyclophilinswhichaidinproteinfolding.CyclosporinA(CsA):cyclophilincomplexestogetherbindcalcineurin,(anothercytosolicprotein)effectivelyblockingthepathwaytoIL-2genetranscriptionandnitricoxidesynthesisbyTNFαandinterleukin1α.
2-8°C
Powder
Whitecrystallinepowder
98.5-101.5%(ondriedbasis)
≤2.0%
≤0.002%
RelatedCompounds:
Individualimpurity:≤0.7%
Totalimpurities:≤1.5%