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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
MW:409.4Da
CASRegistry#:163222-33-1
Formula:C24H21F2NO3
Target:Cholesterolabsorption
Background:
Ezetimibehasbeenreportedtobeacholesteroltransportinhibitor.MechaNISTicstudiesshowthatthiscompounddirectlyaffectsNiemann-PickC1-like1(NPC1L1)andpreventsitfromincorporatingintoclathrin-coatedvesicles.NPC1L1isapolytopictransmembraneproteinthatfacilitatesabsorptionofcholesterolviaclathrin/AP2-mediatedendocytosis.BybindingtoNPC1L1,ezetimibepreventsendocytosisofthisproteinthereforeblockingcholesteroltransferacrossmembranes.Ezetimibeisusedclinicallytolowerplasmacholesterollevels.
Description:
Ezetimibeisananti-hyperlipidemicmedicationwhichisusedtolowercholesterollevels.Specifically,itappearstobindtoacriticalmediatorofcholesterolabsorption,theNiemann-PickC1-Like1(NPC1L1)proteinonthegastrointestinaltractepithelialcellsaswellasinhepatocytes.
Synonym(s):
ezetimibe;Zetia;(3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
BIOLOGicalActivity:
EzetimibeglucuronideinhibitsbromosulfophthaleinuptakeinallOATP-transfectedcellswithanIC50rangingfrom140to260nM.
Solubility:
SolubleinDMSO
Storage/StABIlity:
Storeatorbelow–20°C.Solidformisstableatleast12monthsfromdateofreceipt,whenstoredasdirected.Donotstoreaqueoussolutionsformorethanoneday.
Reference(s):
Garcia-CalvoM,etal.ProcNatlAcadSciUSA.2005Jun7;102(23):8132-7.
ScientificCategory:
Cholesterolinhibitor
ProductType:
Inhibitor
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