Productoverview

• Name
  Compound21(DREADDagoNIST21)
• Shortdescription
  HighlypotenthM3DqDREADDagonist
• BIOLOGicaldescription

  Compound21(DREADDagonist21)isananalogofclozapineN-oxide(CNO). Watersolublehydrochloridesaltalsoavailable.

  
  Compound21(DREADDagonist21)isahighlypotentagonistattheexcitatoryhM3DqDREADD(EC₅₀ =1.7nM)whichshowshighselectivityforactivatinghM3DqcomparedtothenativehM₃ muscarinicreceptorandotherGPCRs.

  
  Compound21hasminimaloff-targetactivity.ThereareindicationsthatCompound21cannotbemetabolizedvianormalroutestoclozapine(oranyrelatedcompound)and thatCompound21hasequivalentpotencyinvivowhencomparedwith clozapineN-oxide.

  UnpublisheddataindicatesthatCompound21(DREADDagonist21)activatestheinhibitoryhM4DDREADD.

  Unpublisheddataalsosuggestsusingadoseof3mg/kginratmodels.

  
  Compound21therefore representsanalternativetoCNO.

• Purity
  >98%
• Ourproductsinaction
  SubmitYourCitationNow

Images

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Properties

• Chemicalname
  11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
• MolecularWeight
  278.35
• Chemicalstructure
  
• MolecularFormula
  C₁₇H₁₈N₄
• CASNumber
  56296-18-5
• PubChemidentifier
  11818276
• SMILES
  C1CN(CCN1)C2=NC3=CC=CC=C3NC4=CC=CC=C42
• Source
  Synthetic
• InChi
  InChI=1S/C17H18N4/c1-2-6-14-13(5-1)17(21-11-9-18-10-12-21)20-16-8-4-3-7-15(16)19-14/h1-8,18-19H,9-12H2
• InChiKey
  JCBYXNSOLUVGTF-UHFFFAOYSA-N
• Appearance
  Yellowsolid

StoringandUsingYourProduct

• Storageinstructions
  RT
• Solubilityoverview
  SolubleinDMSO(100mM)andinethanol(100mM)
• Important
  ThisproductisforRESEARCHUSEONLYandisnotintendedfortherapeuticordiagnosticuse.Notforhumanorveterinaryuse

ReferencesforCompound21(DREADDagonist21)

• Thefirststructure-activityrelationshipstudiesfordesignerreceptorsexclusivelyactivatedbydesignerdrugs.

  Chenetal(2015)ACSChemNeurosci6(3):476-84

  PubMedID:25587888

• OptogeneticapproachesfordissectingneuromodulationandGPCRsignalinginneuralcircuits.

  SpanglerandBruchas(2017)CurrOpinPharmacol32:56-70.

  PubMedID:27875804

• ClozapineN-OxideAdministrationProducesBehavioralEffectsinLong-EvansRats:ImplicationsforDesigningDREADDExperiments.

  MacLarenetal(2016)eNeuro3(5):0219-16

  PubMedID:27822508

• Newnon-CNOactuatorsforDREADDs

  RothBl(2015)Blog:N/A
品牌介绍
Hello Bio是由一群经验丰富的科学家和化学家们创立的充满活力的生物企业，总部位于英国布里斯托尔，在美国普林斯顿设有分公司，主旨在于提供质优价廉的生命科学研究工具，主要产品线为小分子化合物，如激动剂、拮抗剂、抑制剂等，部分产品价格甚至低至其他供应商的50%。热销产品线：酶抑制剂和激动剂ROCK inhibitor Y-27632, PKA inhibitor KT 5720 , adenylyl cyclase activator Forskolin, and novel GRK2/3 inhibitor Cmpd101等。 离子通道调节剂NMDA antagonist D-AP5, sodium channel blocker tetrodotoxin citrate, TRP antagonist capsazepine, and GABAA antagonist SR 95531 等。信号通路工具各种信号通路抑制剂、激动剂表观遗传学研究工具potent HDAC inhibitor Trichostatin A, DNA methyltransferase inhibitor 5-aza-2'-deoxycytidine,BET bromodomain inhibitor (+)-JQ1 and potent,selective GLP / G9a HMTase inhibitor BIX 01294 等受体配体novel selective GRK2/3 inhibitor,  NMDA antagonist D-AP5, Group I mGlu agonist (S)-3,5-DHPG, and GABAA antagonist SR 95531.等干细胞调节剂ROCK inhibitor Y-27632,  SB 431542 DAPT.