品牌分类
品牌咨询
联系方式
公司地址
苏州工业园区生物纳米园A4#216
联系电话
4000-520-616 / 18915418616
传真号码
0512-67156496
电子邮箱
info@ebiomall.com
公司网址
https://www.ebiomall.com
商品描述
| Description | MRE-269(ACT-333679)isaprostaglandinI2(IP)receptoragoNISTwithabindingaffinityforthehumanIPreceptorthatis130-foldgreaterthanthatforotherhumanprostanoidreceptor. | ||
|---|---|---|---|
| Targets |
| ||
| Invitro | MRE-269boundtothehumanIPreceptorwithhighaffinity(bindingaffinity(Ki)of20nM)andwithmorethan130-foldselectivityoverotherprostanoidreceptors(prostaglandinEreceptors,EP1−4;prostaglandinDreceptor,DP1;prostaglandinF2receptor,FP;thromboxaneA2receptor,TP).Inpulmonaryarterialsmoothmusclecells(PASMCs),MRE-269potentlyinducesaccumulationofintracellularcAMP,leadingtolong-lasting(>10h)membranehyperpolarization(EC50=32nM)whichcontributestocellrelaxation.Italsocauseslong-lastingandpronouncedrelaxationofPASMCs[1]. | ||
| Invivo | AfterOralAdministration(1mg/kg)tomonkeys,theTmax(timetoreachmaximumobservedplasmaconcentration),Cmax(maximumobservedplasmaconcentration),AUC0−24h(areaunderthecurvefrom0to24hafterdosing)andT1/2(apparentterminalhalf-life)are2.3h,105ng/mL,652ng·h/mLand5.6h,respectivelyforMRE-269[1]. |
