Pentoxyverine-Carbetapentane-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPentoxyverineCat.No.:HY-134004CASNo.:77-23-6Synonyms:Carbetapentane分⼦式:C₂₀H₃₁NO₃分⼦量:333.47作⽤靶点:SigmaReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(749.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9988mL14.9939mL29.9877mL5mM0.5998mL2.9988mL5.9975mL10mM0.2999mL1.4994mL2.9988mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(6.24mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.24mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.24mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Pentoxyverine(Carbetapentane)sigma-1受体激动剂，在豚⿏脑膜上的Ki值为75nM。Pentoxyverine是⼀种中枢性咳嗽抑制剂，具有抗毒蕈碱和抗惊厥作⽤。Pentoxyverine可⽤于抑制⽀⽓管阻滞剂，减弱咳嗽反射，⽀⽓管平滑肌松弛和降低⽓道阻⼒。IC50&TargetKi:75nM(sigma-1receptor)[4]体外研究Pentoxyverinecompetitivebindsto[3H]-pentazocine-labelledsitesonguinea-pigbrainmembranes,withaKiof75nM[4].体内研究Pentoxyverine(1-5mg/kg;asinglei.p.)inhibitscitric-acid-inducedcoughinguinea-pigs[4].REFERENCES[1].MohamedSH,et,al.Extraction-freespectrophotometricassayoftheantitussivedrugpentoxyverinecitrateusingsulfonephthaleindyes.SpectrochimActaAMolBiomolSpectrosc.2019Nov5;222:117186.[2].TortellaFC,et,al.Dextromethorphanandcarbetapentane:centrallyactingnon-opioidantitussiveagentswithnovelanticonvulsantproperties.BrainRes.1986Sep24;383(1-2):314-8.[3].CalderonSN,et,al.Novel1-phenylcycloalkanecarboxylicacidderivativesarepotentandselectivesigma1ligands.JMedChem.1994Jul22;37(15):2285-91.[4].BrownC,et,al.Antitussiveactivityofsigma-1receptoragonistsintheguinea-pig.BrJPharmacol.2004Jan;141(2):233-40.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresear