Description:ActivatorofmuscarinicDREADDsChemicalName:8-Chloro-11-(4-methyl-4-oxido-1-piperazinyl)-5H-dibenzo[b,e][1,4]diazepinePurity:≥99%(HPLC)BIOLOGicalActivityTechnicalDataSolubilityCalculatorsDatasheetsReferencesBiologicalActivityMetaboliteofclozapine(Cat.No.0444).Activateshumanmuscarinicdesignerreceptors(DREADDs)invitro.SilenceshippocampalneuronsexpressinghM4DREADDsinvitro.ActivatesGs-linkedDREADDS-AgRPinmiceviaintracerebroventricular(i.c.v)injection.ShowntobeaP-glycoprotein(P-gp)effluxpumpsubstrate.Watersolublesalt(Cat.No.6329)alsoavailable.OtherpotentandselectivehM3DqDREADDagoNISTsavailable:DREADDagonist21(Cat.No.5548)andPerlapine(Cat.No.5549)TechnicalDataM.Wt342.82FormulaC18H19ClN4OStorageStoreatRTPurity≥99%(HPLC)CASNumber34233-69-7PubChemID2819InChIKeyWYRDWWAASBTJLM-UHFFFAOYSA-NSmilesClC(C=C3)=CC1=C3NC(C=CC=C2)=C2C(N4CC[N+](C)([O-])CC4)=N1Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.AllTocrisproductsareintendedforlaboratoryresearchuseonly.SolubilityDataSolventMaxConc.mg/mLMaxConc.mMSolubilityDMSO6.8620ethanol3.4310mMwithgentlewarmingPreparingStockSolutionsThefollowingdataisbasedontheproductmolecularweight342.82.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.Concentration/SolventVolume/Mass1mg5mg10mg1mM2.92mL14.58mL29.17mL5mM0.58mL2.92mL5.83mL10mM0.29mL1.46mL2.92mL50mM0.06mL0.29mL0.58mLMolarityCalculatorMolarityCalculatorCalculatethemass,volume,orconcentrationrequiredforasolution.ReconstitutionCalculatorReconstitutionCalculatorDilutionCalculatorDilutionCalculatorCalculatethedilutionrequiredtoprepareastocksolution.ProductDatasheetsCertificateofAnalysis/ProductDatasheetSafetyDatasheetSelectanotherlanguage:EnglishGermanFrenchSpanishViewSDSReferencesReferencesarepublicationsthatsupporttheproducts'biologicalactivity.Eiermannetal(1997)TheinvolvementofCYP1A2andCYP3A4inthemetabolismofclozapine.Br.J.Clin.Pharmacol.44439PMID:9384460Armbrusteretal(2007)EvolvingthelocktofitthekeytocreateafamilyofGprotein-coupledreceptorspotentlyactivatedbyaninertligand.Proc.Natl.Acad.Sci.U.S.A.1045163PMID:17360345Zamanetal(2014)LMO4isessentialforparaventricularhypothalamicneuronalactivityandcalciumchannelexpressiontopreventhyperphagia.J.Neurosci.34140PMID:24381275Gomezetal(2017)Chemogeneticsrevealed:DREADDoccupancyandactivationviaconvertedclozapine.Science357503PMID:28774929Nakajimaetal(2016)Gs-coupledGPCRsignallinginAgRPneuronstriggerssustainedincreaseinfoodintake.Nat.Commun.810268PMID:26743492Rothetal(2016)DREADDsforNeuroscientistsNeuron89683PMID:26889809Keywords:ClozapineN-oxide,supplier,clozapine,metabolite,5HT2A/2C,non-selective,receptors,SEROtonin,5HT2C,5HT2,5HT2A,dopaminergic,dopamine,antagonists,D4,clozapine-N-oxide,DREADDs,DREADD,Ligands,muscarnic,receptors,designer,receptors,CNO,Non-selective,Dopamine,5-HT2A,Receptors,5-HT2C,Receptors,DREADDs,Glutamate,(Metabotropic),Group,III,Receptors,Glutamate,(Metabotropic),Group,II,Receptors,Multidrug,Transporters,DREADDs,TocrisBioscience
Tocris Bioscience是一家专卖生命科学研究chemicals, peptides and antibodies的知名品牌,其产品也广为各大药厂、大学、研究机构,超过五万名科学研究者所采用。 目前,產品內容已超過一千六百種以上,並每年持續不斷的增加新的產品。目前,产品内容已超过一千六百种以上,并每年持续不断的增加新的产品。
Tocris bioscience是位于英国布里斯托尔(Bristol)的高品质试剂提供商,共有2000多种产品,主要集中在神经科学和信号传导领域,产品类型包括小分子、多肽、抗体、配体和化合物筛选文库等,主要产品包括GPCR ligands,神经传递素,离子通道调控剂,信号通路抑制剂等,这些产品被广泛选择性地用于阻断或激活生物学通路。Tocris是世界上神经科学研究领域无可争议的领导者,其生产的影响神经系统的化学物质被多次引用,这些物质很多都来自Jeff Watkins(Tocris 的创立人)在Bristol大学原创性的研究工作。
Tocris Bioscience的主要产品包括:
Small Molecules
Peptides
Aptamers
Controlled Substances
Compound Libraries
DREADD Ligands
Fluorescent Imaging
Ligand Sets
Optopharmacology
Reagents
Toxins
按照研究领域细分:
Cancer
Cardiovascular System
Endocrinology
Immunology
Neuroscience
Pain & Inflammation
Respiratory System