OD1isascorpionpeptidethathasbeenisolatedinitiallyfromthevenomofthescorpionOdonthobuthusdoriae.OD1potentlyinhibitsfastinactivationofmammalianchannelsNav1.7(EC504.5nM),Nav1.4(EC5010±2nM)andNav1.6(EC5047±10nM). OD1 alsoblocksfastinactivationofthepara/tipEinsectchannel(EC5080nM).OD1weaklyaffectsmammalianNav1.3andNav1.5(EC50>1μM)anddoesnotaffectNav1.2andNav1.8. OD1inducesspontaneouspainwheninjectedinanimalinassociationwithourwithout VeratridineandcanbeusedtotesttheanalgesiceffectsofNav1.7blockersin-vivo.
A,C,TimecourseofthemodulatingeffectofOD1#ODX001(50nM)onhNav1.7current. Thecurrentwaselicitedbya50ms-depolarizingpulseto-25mV(estimatedV1/2)orto-10mVfromaholdingpotentialof-90mV.Inter-sweepperiodwas10s.Currentamplitudeswereplottedagainsttime.Blackbarindicatestoxinapplication.B,D,RepresentativerecordingtracesofNav1.7currentincontrolcondition(black)andaftertheeffectofOD1#ODX001hadstABIlized(red).Theinactivationkineticsofcurrentwasfittedwiththestandardmono-exponentialfunction.E,FamiliesofhNav1.7currenttracesincontrolandinthepresenceof50nMOD1#ODX001.Currentswereevokedbydepolarizingpulsesfrom-60mVto40mV,whilethecellwasholdat-90mV.F,Amplitude-voltagerelationshipsobtainedfromE.
RecentlyquotedDescription:
AAsequence: GVRDAYIADDKNCVYTCASNGYCNTECTKNGAESGYCQWIGRYGNACWCIKLPDEVPIRIPGKCR-NH2
Disulfidebonds: C13-C64 ;C17-C37 ;C23-C47 ;C27-C49
Length(aa):65
Formula: C308H466N90O95S8
Appearance:Whitelyophilizedsolid
CASnumber:Notavailable
MolecularWeight:7206.20Da
Source:Synthetic
Counterion:TFAsalts
Solubility:Waterorsalinebuffer,5mg/mLmaximum(recommendation)
Purity:>95%
