Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPentoxyverineCat.No.:HY-134004CASNo.:77-23-6Synonyms:Carbetapentane分?式:C??H??NO?分?量:333.47作?靶點(diǎn):SigmaReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(749.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.9988mL14.9939mL29.9877mL5mM0.5998mL2.9988mL5.9975mL10mM0.2999mL1.4994mL2.9988mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(6.24mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.24mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.24mM);ClearsolutionBIOLOGICALACTIVITY?物活性Pentoxyverine(Carbetapentane)sigma-1受體激動(dòng)劑，在豚?腦膜上的Ki值為75nM。Pentoxyverine是?種中樞性咳嗽抑制劑，具有抗毒蕈堿和抗驚厥作?。Pentoxyverine可?于抑制??管阻滯劑，減弱咳嗽反射，??管平滑肌松弛和降低?道阻?。IC50&TargetKi:75nM(sigma-1receptor)[4]體外研究Pentoxyverinecompetitivebindsto[3H]-pentazocine-labelledsitesonguinea-pigbrainmembranes,withaKiof75nM[4].體內(nèi)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