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Tocris/SR 144528/5039/50/50 mg
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Description:HighaffinityandselectiveCB2inverseagoNISTChemicalName:5-(4-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamidePurity:≥98%(HPLC)BIOLOGicalActivityTechnicalDataSolubilityCalculatorsDatasheetsReferencesBiologicalActivityHighaffinityandselectiveCB2inverseagonist(Ki=0.6nM).Exhibits>700-foldselectivityforCB2overCB1receptors.BlockstheeffectsofCP55,940(Cat.No.0949)onforskolin-sensitiveadenylylcyclaseactivityandMAPKinCHOcellsexpressingCB2receptors.AlsoblocksCP55,940-inducedB-cellactivation.Orallybioavailable.TechnicalDataM.Wt476.05FormulaC29H34ClN3OStorageStoreat-20°CPurity≥98%(HPLC)CASNumber192703-06-3PubChemID3081355InChIKeySUGVYNSRNKFXQM-XRHWURSXSA-NSmilesC[C@]1(C2)[C@H](NC(C3=NN(CC4=CC=C(C)C=C4)C(C5=CC=C(Cl)C(C)=C5)=C3)=O)C(C)(C)[C@@H]2CC1Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.AllTocrisproductsareintendedforlaboratoryresearchuseonly.SolubilityDataSolventMaxConc.mg/mLMaxConc.mMSolubilityDMSO47.6100ethanol47.6100PreparingStockSolutionsThefollowingdataisbasedontheproductmolecularweight476.05.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.Concentration/SolventVolume/Mass1mg5mg10mg1mM2.1mL10.5mL21.01mL5mM0.42mL2.1mL4.2mL10mM0.21mL1.05mL2.1mL50mM0.04mL0.21mL0.42mLMolarityCalculatorMolarityCalculatorCalculatethemass,volume,orconcentrationrequiredforasolution.ReconstitutionCalculatorReconstitutionCalculatorDilutionCalculatorDilutionCalculatorCalculatethedilutionrequiredtoprepareastocksolution.ProductDatasheetsCertificateofAnalysis/ProductDatasheetSafetyDatasheetSelectanotherlanguage:EnglishGermanFrenchSpanishViewSDSReferencesReferencesarepublicationsthatsupporttheproducts'biologicalactivity.Rinaldi-Carmonaetal(1998)SR144528,thefirstpotentandselectiveantagonistoftheCB2cannABInoidreceptor.J.Pharmacol.Exp.Ther.284644PMID:9454810Kotsikorouetal(2013)TheimportanceofhydrogenbondingandaromaticstackingtotheaffinityandefficacyofcannabinoidreceptorCB2antagonist,5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethJ.Med.Chem.566593PMID:23855811Bouaboulaetal(1999)GiproteinmodulationinducedbyaselectiveinverseagonistfortheperipheralcannabinoidreceptorCB2:implicationforintracellularsignalizationcross-regulation.Mol.Pharmacol.55473PMID:10051530Keywords:SR144528,supplier,SR144528,high,affinity,selective,cannabinoid,receptors,CB2,inverse,agonists,orally,bioavailable,immunology,CB2,Receptors,CB2,Receptors,TocrisBioscience

Tocris Bioscience.png


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


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