Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVigabatrinCat.No.:HY-15399CASNo.:68506-86-5Synonyms:γ-Vinyl-GABA分?式:C?H??NO?分?量:129.16作?靶點:GABAReceptor作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗H2O:50mg/mL(387.12mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM7.7423mL38.7117mL77.4233mL5mM1.5485mL7.7423mL15.4847mL10mM0.7742mL3.8712mL7.7423mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：PBS1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:100mg/mL(774.23mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Vigabatrin(γ-Vinyl-GABA)，?種抑制性神經遞質GABA?烯衍?物，?種具有?服活性且不可逆的GABA轉氨酶(GABAtransaminase)抑制劑。Vigabatrin?種抗癲癇劑，通過抑制GABAtransaminase對GABA的分解代謝來增加腦中GABA的?平。體外研究Asignificantincreaseinseizurethresholdisobservedfollowingsystemic(i.p.)administrationofhigh(600or1200mg/kg)dosesofVigabatrin.BilateralmicroinjectionofVigabatrin(10μg)intoeithertheanteriororposteriorsubstantianigraparsreticulata(SNr)alsoincreasedseizurethreshold,butlessmarkedlythansystemictreatment.Focaldeliveryintothesubthalamicnucleus(STN)increasedseizurethresholdmoremarkedlythaneitherintranigralorsystemicadministrationofVigabatrin[1].體內研究VigabatrininhibitstheuptakeoftaurineinCaco-2andMDCKcellsto34%and53%,respectively,ataconcentrationof30mM.InCaco-2cellstheuptakeofVigabatrinunderneutralpHconditionsisconcentration-dependentandsaturablewithaKm-valueof27mM.Vigabatrinisabletoinhibittheuptakeoftaurineinintestinalandrenalcellculturemodels[2].戶使?本產品發表的科研?獻?RedoxBiol.2021Jul26;46:102082.?JExpBot.2020Feb19;71(4):1459-1474.?Plants.2020Apr3;9(4):449.?Animals.2020Mar27;10(4):567.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Broeer,etal.Vigabatrinforfocaldrugdeliveryinepilepsy:Bilateralmicroinfusionintothesubthalamicnucleusismoreeffectivethanintranigralorsystemicadministrationinaratseizuremodel.NeurobiologyofDisease(2012),46(2),362-376.[2].Gaily,EijaVigabatrinmonotherapyforinfantilespasms.ExpertReviewofNeurotherapeutics(2012),12(3),275-286.[3].JakobPlum,etal.Theanti-epilepticdrugsubstancevigabatrininhibitstaurinetransportinintestinalandrenalcellculturemodels.IntJPharm.2014Oct1;473(1-2):395-7.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical