ProductDescription
Plerixafor(AMD3100)isabis-tetraazadecane-based,selectiveinhibitorofhumanimmunodeficiencyvirus.ItisinhibitorytothereplicationofvariousHIV-1andHIV-2strainsinvariouscelllinesatanEC50of1-10ng/mL,about100,000-foldlowerthancytotoxicconcentrations(>500uM/mL).[1]PlerixaforshowsinhibitiontoHIV-1(IIIB)andseveralclinicalHIV-1isolatesatanEC50oflessthan1ng/mL.
PlerixaforhasbeenshowntobeactiveinHIVstrainsresistanttoreversetranscriptaseinhibitorsAZT,DDI,3TC,aAPA,andTIBO.[2]
PlerixaforblocksHIV-1entryandmembranefusionviatheCXCR4co-receptor,butnotviaCCR5.Italsopreventsmonoclonalantibody12G5frombindingtoCXCR4.EntryintoCXCR-expressingcellswasstronglyinhibitedbyPlerixaforatIC50valuesof0.01-0.1nM.[3]PlerixafordemonstratesaspecificantagonismoftheinteractionbetweenchemokineSDF-1andCXCR4,reducingseverityofinflammationinCIAmodels.[4]
Technicalinformation:
ChemicalFormula: | C28H54N8 | |
CAS#: | 110078-46-1,155148-31-5 | |
MolecularWeight: | 502.78 | |
Purity: | >98% | |
Appearance: | White | |
ChemicalName: | 1,1"-[1,4-PhenyleNEBis(methylene)]bis[1,4,8,11-tetraazacyclotetradecane] | |
Solubility: | Upto100mMinwaterinDMSO | |
Synonyms: | AMD3100,AMD3100,Plerixafor,Mozobil,bicyclamJM-2987 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
1. | DeClercqetal.,HighlypotentandselectiveinhibitionofhumanimmunodeficiencyvirusbythebicyclamderivativeJM3100.Antimicrob.AgentsChemother.1994,38(4),668-674.PubmedID:7913308 |
2. | Esteetal.,AntiviralactivityofthebicyclamderivativeJM3100againstdrug-resistantstrainsofhumanimmunodeficiencyvirustype1.AntiviralRes.1996,29,297-307.PubmedID:8739608 |
3. | Donzellaetal.,AMD3100,asmallmoleculeinhibitorofHIV-1entryviatheCXCR4co-receptor.NatureMed.1998,4(1),72-77.PubmedID:9427609 |
4. | Matthysetal.,AMD3100,apotentandspecificantagoNISTofthestromalcell-derivedfactor-1chemokinereceptorCXCR4,inhibitsautoimmunejointinflammationinIFN-gammareceptor-deficientmice.J.Immunol.2001,167(8),4686-4692.PubmedID:8739608 |