MolecularWeight: | 441.52 |
Formula: | C26H27N5O2 |
Purity: | ≥98% |
CAS#: | 700874-71-1 |
Solubility: | DMSOupto100mM |
ChemicalName: | 4-(2-((4-(2-(pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinolin-7-yl)oxy)ethyl)morpholine |
Storage: | Powder:4oC1year.DMSO:4oC3month;-20oC1year. |
BIOLOGicalActivity:
LY2109761isahighlypotentandselectiveTGFβreceptortypeIandtypeII(TβRI/II)inhibitorwithKiof38nMand300nMrespectively.BlockingTβRI/IIkinaseactivitywithLY2109761completelysuppressesboththebasalandTGF-β1-stimulatedmigrationandinvasionofL3.6pl/GLTcells,andcompletelysuppressesTGF-β–inducedSmad2phosphorylation.LY2109761treatmentat1nMissufficienttosignificantlyblockthemigrationandinvasionbutnotadhesionofhepatocellularcarcinomacellsbyincreasingE-cadherinexpression.Itcanalsoreducetheself-renewalandproliferationofGBM-derivedcancerstem–likecells,whichcanbesignificantlyenhancedwhencombinedwithrADIation.AdmiNISTrationofLY2109761aloneorincombinationwithgemcitABIneorwithradiationdemonstratedverygoodefficacyinmultiplexenograftmicemodels.
HowtoUse:
- Invitro:LY2109761wasusuallyusedat5-10µMinvitroandincellularassays.
- Invivo:LY2109761wasorallydosedtomiceat50mg/kgonceperdayorincombinationwithgemcitabine(25mg/kg)tosignificantlyreducethetumorvolume.
Reference:
- 1.LiHY,etal.Optimizationofadihydropyrrolopyrazoleseriesoftransforminggrowthfactor-betatypeIreceptorkinasedomaininhibitors:discoveryofanorallybioavailabletransforminggrowthfactor-betareceptortypeIinhibitorasantitumoragent.(2008)JMedChem.51(7):2302-6.
- 2.MelisiD,etal.LY2109761,anoveltransforminggrowthfactorbetareceptortypeIandtypeIIdualinhibitor,asatherapeuticapproachtosuppressingpancreaticcancermetastasis.(2008)MolCancerTher.7(4):829-40.
- 3.ZhangB,etal.Targetingtransforminggrowthfactor-betasignalinginlivermetastasisofcoloncancer.(2009)CancerLett.277(1):114-20.
- 4.ConnollyEC,etal.Outgrowthofdrug-resistantcarcinomasexpressingMarkersoftumoraggressionafterlong-termTβRI/IIkinaseinhibitionwithLY2109761.(2011)CancerRes.71(6):2339-49.
- 5.ZhangM,etal.BlockadeofTGF-βsignalingbytheTGFβR-IkinaseinhibitorLY2109761enhancesradiationresponseandprolongssurvivalinglioblastoma.(2011)CancerRes.71(23):7155-67.
- 6.FlechsigP,etal.LY2109761AttenuatesRadiation-InducedPulmonaryMurineFibrosisviaReversalofTGF-βandBMP-AssociatedProinflammatoryandProangiogenicSignals.(2012)ClinCancerRes.18(13):3616-27
- LY2109761_spec.pdf
- LY2109761_MSDS_1.pdf
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MaggotsFasterThanScalpelinWoundDebridement
December19,2011—Maggotdebridementtherapy(MDT)appearstobemoreeffectiveforwounddebridementcomparedwithconventionaltherapy,butonlyat1week;afterthattime,anothertypeofdressingshouldbeused,newresearchsuggests.
KristinaOpletalovà,MD,fromtheDepartmentofDermatology,UniversityofCaen,France,andcolleaguespublishedonlineDecember19intheArchivesofDermatology.
MedicalmaggotswereapprovedbytheUSFoodandDrugAdmiNISTrationasamedicaldeviceforwounddebridementin2004.Accordingtotheresearchers,useofmaggotsintreatingwoundsisassociatedwitheffectivewounddebridement,antibacterialeffects,andstimulationofwoundhealing.
However,theypointout,"[r]elativelyfewclinicalstudieshavebeenconductedandtheresultsarenotclear,partlyowingtomethodologicassessmentproblems."
InthecurrentProspective,randomizedcontrolled,phase3clinicaltrial,theresearcherssoughttodeterminetheefficacyofbaggedlarvaeonwounddebridementincomparisonwithconventionaltreatment.
TheprimaryobjectivewastocomparethemeanpercentageofsloughinwoundstreatedwithMDTwiththatofconventionaltreatmentatday15.Thestudyincluded119patientswithanonhealing,sloughywoundthatwas40cm2orsmallerandlessthan2cmdeep.Patientsalsohadananklebrachialindexof0.8orhigher.
Treatmentwasadministeredduringa2-weekhospitalstay.Conventionaltreatmentconsistedofsurgicaldebridement3timesaweekwithascalpel,withuseoftopicalanesthesia.TheMDTwasadministeredusinganencloseddressing(Vitapad,BioMondeLaboratories)containing80sterilemaggots.Atdischarge,aconventionaldressingwasapplied,andpatientswerefollowed-upatday30.
DebridementbyMDTwassignificantlyfasterthansurgicaldebridementduringthefirstweekoftreatment,reachingthesamelevelthecontrolgroupreachedatday15.NobenefitforMDTcomparedwithconventionaltreatmentinhealingrateswasobserved.Atday8,54.5%intheMDTgroupvs66.5%inthecontrolgroup(P=.04)hadevidenceofsloughandwoundhealing.However,byday15,themeanpercentageofsloughwas55.4%intheMDTgroupand53.8%inthecontrolgroup(P=.78).
"AthoughMDTshowsnosignificantbenefitatday15comparedwithconventionaltreatment,debridementbyMDTissignificantlyfasterandoccursduringthefirstweekoftreatment,"theresearchersconclude."Becausethereisnobenefitincontinuingthetreatmentafter1week,anothertypeofdressingshouldbeusedafter2or3applicationsofMDT."
Painscoresweresimilarandmildinbothgroups,althoughincontrasttoconventionaltreatment,MDTwasperformedwithouttopicalanesthesia.
Accordingtotheresearchers,noneofthepatientswerereticentaboutundergoingMDT."[A]crawlingsensationonthewoundwasrarelyandalmostequallynotedinbothgroups,revealingthatthesensationwassubjective,"Dr.Opletalovàandcolleaguespointout.
TwoquestionsregardingMDTremainunanswered,theauthorsnote."Candebridementbeimprovedusingmoremaggotsperdressing?Ifso,wouldthesedressingsbemorepainful?Furtherstudiesareneededtoanswerthesequestions."
ThestudywassupportedbygrantsfromtheClinicalResearchHospitalProgramandfromtheFrenchSocietyofDermatology.Theauthorshavedisclosednorelevantfinancialrelationships.
1. 姜黄素是一个典型的HAT抑制剂。
2. 针对P300: 在大约10年前,Cole和他的同事设计出了一种p300/CBP抑制剂,发表在nature杂志上。
希望能帮到你,望采纳!
天然产物,大多都有颜色,
存在干扰,多数情况下需要做样品的阴性对照,
尽量能用荧光的方法,
之前我们做过,将两个试剂盒的方法合并后,做的,
效果还可以
支原体培养则是取样后在培养基上培养,看有多少支原体菌落会长出,是比较直观和可信的结果。
总体来讲,这两种检查手段可信度都较高,结合一起,不仅可以可靠的知道有无解脲支原体感染,还能知道感染是否严重。