Heparin(sodiumsalt)isahighlysulfatedglycosaminoglycan,thatiswidelyusedasaninjectableanticoagulant,andhasthehighestnegativechargedensityofanyknownbiologicalmolecule.

HeparinisapotentanticoagulantdrugbasedonitsABIlitytoacceleratetherateatwhichantithrombininhibitsserineproteasesinthebloodcoagulationcascade.Heparinandthestructurallyrelatedheparansulfatearecomplexlinearpolymerscomprisedofamixtureofchainsofdifferentlength,havingvariablesequences.Heparininteractesmosttightlywithpeptidescontainingacomplementarybindingsiteofhighpositivechargedensity.Heparinandheparansulfatepredominantlyexhibitlinearhelicalsecondarystructureswithsulfoandcarboxylgroupsdisplayedatdefinedintervalsandindefinedorientationsalongthepolysaccharidebackbone.HeparinresemblesDNAasbotharehighlychargedlinearpolymersthatbehaveaspolyelectrolytes.HeparinisbelievedtofunctionasananticoagulantprimarilythroughitsinteractionwithATIIIbyenhancingAT-III-mediatedinhibitionofbloodcoagulationfactors,includingthrombinandfactorXa.HeparinbindstoATIIIandthrombininaternarycomplex,increasingthebimolecularrateconstantfortheinhibitionofthrombinbyafactorof2000.Heparinisprincipallylocatedinthegranulesoftissuemastcellsthatarecloselyassociatedwiththeimmuneresponse.HeparinmakesnumerouscontactswithbothFGF-2andFGFR-1stabilizingFGF–FGFRbinding.HeparinalsomakescontactswiththeFGFR-1oftheadjacentFGF–FGFRcomplex,thusseemingtopromoteFGFRdimerization^[1].

• [1].CapilaI,etal.Heparin-proteininteractions.AngewChemIntEdEngl.2002Feb1;41(3):391-412.

1157.92

C₂₆H₄₂N₂NaO₃₇S₅+

9041-08-1

RoomtemperatureincontinentalUS;mayvaryelsewhere

H₂O:≥32mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">