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Smartox/OD1, a potent Nav1.7 channel activator/ODX001-00500/0.5mg
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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:Productcode:N/A.Category:Sodiumchannels.Tags:nav1.3,nav1.6,Nav1.7,pain.AAsequence: GVRDAYIADDKNCVYTCASNGYCNTECTKNGAESGYCQWIGRYGNACWCIKLPDEVPIRIPGKCR-NH2Disulfidebonds: C13-C64 ;C17-C37 ;C23-C47 ;C27-C49Length(aa):65Formula: C308H466N90O95S8Appearance:WhitelyophilizedsolidCASnumber:NotavailableMolecularWeight:7206.20DaSource:SyntheticCounterion:TFAsaltsSolubility:Waterorsalinebuffer,5mg/mLmaximum(recommendation)Purity:>95%
Smartox Biotechnology 是全球唯一一家专门生产动物毒液多肽毒素,用于细胞离子通道功能研究的生物医药公司。多肽毒素在生物制药领域具有重要的使用价值。Smartox Biotechnology 于 2009 年由来自 Grenoble 神经科学研究所 (Grenoble Institute of Neuroscience) 的 Michel de waard 博士创立, Smartox Biotechnology 专门研究动物毒液,制作合成多种毒液中的多肽成分(常称为毒素)。 De Waard 博士研究离子通道与毒素多肽的关系,尤其是鉴定、开发毒素多肽作为治疗性分子或细胞穿透肽 (cell penetrating peptides, CPP) 。其研究团队在毒液分离,药理性活性肽鉴定、富半胱氨酸肽定性、制作和优化等方面具有独特、丰富的经验。 2010 年, Smartox Biotechnolgy 被法国研究部 (Ministry of Research) 授予“新兴企业 OSEO 奖 (OSEO prize for emerging businesses) ”。
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