MedKooCat#:200700
Name:Celecoxib
CAS#:169590-42-5
ChemicalFormula:C17H14F3N3O2S
ExactMass:381.07588
MolecularWeight:381.37
ElementalAnalysis:C,53.54;H,3.70;F,14.94;N,11.02;O,8.39;S,8.41
Synonym:
IUPAC/ChemicalName:4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide
InChiKey:RZEKVGVHFLEQIL-UHFFFAOYSA-N
InChiCode:InChI=1S/C17H14F3N3O2S/c1-11-2-4-12(5-3-11)15-10-16(17(18,19)20)22-23(15)13-6-8-14(9-7-13)26(21,24)25/h2-10H,1H3,(H2,21,24,25)
SMILESCode:O=S(C1=CC=C(N2N=C(C(F)(F)F)C=C2C3=CC=C(C)C=C3)C=C1)(N)=O
TechnicalData
AdditionalInformation
Celecoxibisasulfanon-steroidalanti-inflammatorydrug(NSAID)usedinthetreatmentofosteoarthritis,rheumatoidarthritis,acutepain,painfulmenstruationandmenstrualsymptoms,andtoreducenumbersofcolonandrectumpolypsinpatientswithfamilialadenomatouspolyposis.ItismarketedbyPfizer.ItisknownunderthebrandnameCelebrexorCelebraforarthritisandOnsenalforpolyps.Celecoxibisavailablebyprescriptionincapsuleform.
PfizersellscelecoxibunderthebrandnameCelebrex.CelecoxibisnotcurrentlyavailableasagenericintheUnitedStates,becausetheintellectualpropertyisstillcontrolledbyPfizer.However,inothercountries,includingIndiaandthePhilippines,itislegallyavailableasagenericunderthebrandnamesCobixandCelcoxx.XLLaboratoriessellscelecoxibunderthebrandnameSelecapinVietnamandthePhilippines.Seehttp://en.wikipedia.org/wiki/Celecoxib.
History
Afterthewithdrawalofrofecoxib(Vioxx)fromthemarketinSeptember2004,Celebrexenjoyedarobustincreaseinsales.However,theresultsoftheAPCtrialinDecemberofthatyearraisedconcernsthatCelebrexmightcarryriskssimilartothoseofVioxx,andPfizerannouncedamoratoriumondirect-to-consumeradvertisingofCelebrexsoonafterwards.Afterasignificantdrop,salesofCelebrexhaverecovered,andreached$2billionin2006. PfizerresumedadvertisingCelebrexinmagazinesin2006, andresumedtelevisionadvertisinginApril2007withanunorthodox,2Å“minuteadvertisementwhichextensivelydiscussedtheadverseeffectsofCelebrexincomparisonwithotheranti-inflammatorydrugs.TheaddrewcriticismfromtheconsumeradvocacygroupPublicCitizen,whichcalledthead'scomparisonsmisleADIng.PfizerhasrespondedtoPublicCitizen'sconcernswithassurancesthattheyaretruthfullyadvertisingtheriskandbenefitsofCelebrexassetforthbytheFDA.Inlate2007,PfizerreleasedanotherU.S.televisionadforCelebrex,whichalsodiscussedcelecoxib'sadverseeffectsincomparisonwiththoseofotheranti-inflammatorydrugs.Dr.SimmonsofBrighamYoungUniversity,whodiscoveredtheCOX-2enzyme,issuingPfizertobecreditedwithdiscoveryofthetechniquein1989thateventuallyledtothedrug,andfor$1billionUSD,(Thecompanyhasmadeabout$30billionfromthedrugasof2006).
Researchintocancerprevention
Therolethatcelecoxibmighthaveinreducingtheratesofcertaincancershasbeenthesubjectofmanystudies.However,giventhesideeffectsofanti-COX-2onratesofheartdisease,thereisnocurrentmedicalrecommendationtousethisdrugforcancerreduction.ColorectalcancerriskisclearlyreducedinpeopleregularlytakingaNSAIDlikeaspirinorcelecoxib.Inaddition,someepidemiologicalstudies,andmostpreclinicalstudiespointedoutthatspecificCOX-2inhibitorslikecelecoxibaremorepotentandlesstoxicthan"older"NSAIDs.Twelvecarcinogenesisstudiessupportthatcelecoxibisstrikinglypotenttopreventintestinalcancerinratsormice(dataavailableontheChemopreventionDatabase).Small-scaleclinicaltrialsinveryhighriskpeople(belongingtoFAPfamilies)alsoindicatethatcelecoxibcanpreventpolypgrowth.Hencelarge-scalerandomizedclinicaltrialswereundertakenandresultspublishedbyN.ArberandM.BertagnolliintheNewEnglandJournalofMedicine,August2006.Resultsshowa33to45%polyprecurrencereductioninpeopletaking400–800mgcelecoxibeachday.However,seriouscardiovasculareventsweresignificantlymorefrequentinthecelecoxib-treatedgroups(seeabove,cardiovasculartoxicity).Aspirinshowsasimilar(andpossIBLylarger)protectiveeffect,hasdemonstratedcardioprotectiveeffectsandissignificantlycheaper,buttherehavebeennohead-to-headclinicaltrialscomparingthetwodrugs.
Researchintocancertreatment
Differentfromcancerprevention,cancertreatmentisfocusedonthetherapyoftumorsthathavealreadyformedandhaveestablishedthemselvesinsidethepatient.Manystudiesareongoingtodeterminewhethercelecoxibmightbeusefulforthislattercondition.However,duringmolecularstudiesinthelaboratory,itbecameapparentthatcelecoxibcouldinteractwithotherintracellularcomponentsbesidesitsmostfamoustarget,cyclooxygenase2(COX-2).Thediscoveryoftheseadditionaltargetshasgeneratedmuchcontroversy,andtheinitialassumptionthatcelecoxibreducestumorgrowthprimarilyviatheinhibitionofCOX-2becamecontentious.Certainly,theinhibitionofCOX-2isparamountfortheanti-inflammatoryandanalgesicfunctionofcelecoxib.However,whetherinhibitionofCOX-2alsoplaysadominantroleinthisdrugÂ’santicancereffectsisunclear.Forexample,arecentstudywithmalignanttumorcellsshowedthatcelecoxibcouldinhibitthegrowthofthesecellsinvitro,butCOX-2playednoroleinthisoutcome;evenmorestrikingly,theanticancereffectsofcelecoxibwerealsoobtainedwiththeuseofcancercelltypesthatdonÂ’tevencontainCOX-2.AdditionalsupportfortheideathatothertargetsbesidesCOX-2areimportantforcelecoxib'santicancereffectshascomefromstudieswithchemicallymodifiedversionsofcelecoxib.Severaldozenanalogsofcelecoxibweregeneratedwithsmallalterationsintheirchemicalstructures.SomeoftheseanalogsretainedCOX-2inhibitoryactivity,whereasmanyothersdidn't.However,whentheABIlityofallthesecompoundstokilltumorcellsincellculturewasinvestigated,itturnedoutthattheantitumorpotencydidnotatalldependonwhetherornottherespectivecompoundcouldinhibitCOX-2,showingthatinhibitionofCOX-2wasnotrequiredfortheanticancereffects. Oneofthesecompounds,2,5-dimethyl-celecoxib,whichentirelylackstheabilitytoinhibitCOX-2,actuallyturnedouttodisplaystrongeranticanceractivitythancelecoxibitself.
Currentdeveloper: Pfizer
References
1:DerryS,MooreRA.Singledoseoralcelecoxibforacutepostoperativepaininadults.CochraneDatabaseSystRev.2012Mar14;3:CD004233.Review.PubMedPMID:22419293.
2:WinfieldLL,Payton-StewartF.CelecoxibandBcl-2:emergingpossibilitiesforanticancerdrugdesign.FutureMedChem.2012Mar;4(3):361-83.Review.PubMedPMID:22393942;PubMedCentralPMCID:PMC3398981.
3:McCormackPL.Celecoxib:areviewofitsuseforsymptomaticreliefinthetreatmentofosteoarthritis,rheumatoidarthritisandankylosingspondylitis.Drugs.2011Dec24;71(18):2457-89.doi:10.2165/11208240-000000000-00000.Review.PubMedPMID:22141388.
4:ArakawaY,NakaiN,KatohN.Celecoxib-inducederythemamultiforme-typedrugeruptionwithapositivepatchtest.JDermatol.2011Dec;38(12):1185-8.doi:10.1111/j.1346-8138.2010.01182.x.Epub2011Mar21.Review.PubMedPMID:22103805.
5:MallenSR,EssexMN,ZhangR.GastrointestinaltolerabilityofNSAIDsinelderlypatients:apooledanalysisof21randomizedclinicaltrialswithcelecoxibandnonselectiveNSAIDs.CurrMedResOpin.2011Jul;27(7):1359-66.Epub2011May12.Review.PubMedPMID:21561397.
6:SakamotoC,SoenS.Efficacyandsafetyoftheselectivecyclooxygenase-2inhibitorcelecoxibinthetreatmentofrheumatoidarthritisandosteoarthritisinJapan.Digestion.2011;83(1-2):108-23.Epub2010Nov1.Review.PubMedPMID:21042022.
7:AmriteA,PugazhenthiV,CheruvuN,KompellaU.Deliveryofcelecoxibfortreatingdiseasesoftheeye:influenceofpigmentanddiabetes.ExpertOpinDrugDeliv.2010May;7(5):631-45.Review.PubMedPMID:20205602;PubMedCentralPMCID:PMC2858240.
8:DuboisRN.New,long-terminsightsfromtheAdenomaPreventionwithCelecoxibTrialonapromisingbuttroubledclassofdrugs.CancerPrevRes(Phila).2009Apr;2(4):285-7.Epub2009Mar31.Review.PubMedPMID:19336723.
9:FakihMG,RustumYM.Doescelecoxibhavearoleinthetreatmentofpatientswithcolorectalcancer?ClinColorectalCancer.2009Jan;8(1):11-4.Review.PubMedPMID:19203891.
10:O'ConnorJP,LyszT.Celecoxib,NSAIDsandtheskeleton.DrugsToday(Barc).2008Sep;44(9):693-709.Review.PubMedPMID:19137124.
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中文名MedKoo中 文美帝药库医药科技公司创立于2008年总部位于美国东海岸
MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。 MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务和分子有竞争力的价格。MedKoo是您可靠的合作伙伴采购药物发现和药物分子。 MedKoo是世界的抗癌化学试剂和激酶抑制剂供应商之一。我们制造,销售和分销用于肿瘤学研究的高质量抗癌小分子试剂。我们的使命是建立世界上全面的抗癌小分子集合。我们还为制药行业,医学研究组织和学术机构提供高质量的研究服务。我们致力于以具有竞争力的价格提供服务和分子。MedKoo是您可靠的药物发现和药物分子采购合作伙伴。 CRISPR-Cas9是近年兴起的用于靶向基因组特定位置,进行DNA修饰的重要工具。研究发现CRISPR是细菌为了应对病毒的攻击而演化而来的获得性免疫防御机制。具体来说,在CRISPR和Cas9的作用下,经由小RNA分子的引导,靶向并沉默入侵者遗传物质核酸的关键部分。在该系统中,crRNA(CRISPR-derivedRNA)与tracrRNA(trans-activatingRNA)结合形成的复合物能特异性识别靶基因序列,并引导Cas9核酸内切酶在靶定位点剪切双链DNA,随后,细胞的非同源末端连接修复机制(NHEJ)重新连接断裂处的基因组DNA,并引入插入或缺失突变。另外也可以提供一个外源双链供体DNA(Donor)通过同源重组(HR)整合进断裂处的基因组,从而达到对基因组DNA进行修饰的目的。
目前,CRISPR-Cas9系统的高效基因组编辑功能已被应用于多种生物,包括小鼠、大鼠、斑马鱼、秀丽隐杆线虫,也包含多种细菌和植物,甚至在人体上也有应用。
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2.NaHCO3,Ba(OH)3,H2SO4
3.HCL,NaAlO2,NaHSO4
4.Ca(OH)2,Na2CO3,BaCO3
谢谢了
要原因
请问有什么方法检测细胞内活性氧更好,各位有什么经验,及相关试剂盒推荐一下。
A.H2SO4Na2SO4AgNO3BaCl2.
B.NaOHNa2CO3NaHSO4MgCl2
C.CaCl2NaNO3MgSO4BaCl2
D.HNO3KOHKClK2CO3
请问下有无同学需要H37RA的?我是做EAE模型的,上个月购买了BDDifco公司的H37RA(货号),因为购买的时候只能整盒6支购买,但我们用不了那么多,所以想问问有无同学需要的,100mg/支,800元/支或用等价试剂交换。地址广州。有需要的请私信,谢谢!
(1)优级纯试剂 亦称保证试剂,为一级品,纯度高,杂质极少,主要用于精密分析和科学研究,常以GR表示。
(2)分析纯试剂 亦称分析试剂,为二级品,纯度略低于优级纯,杂质含量略高于优级纯,适用于重要分析和一般性研究工作,常以AR表示。
(3)化学纯试剂 为三级品,纯度较分析纯差,但高于实验试剂,适用于工厂、学校一般性的分析工作,常以CP表示。
(4)实验试剂 为四级品,纯度比化学纯差,但比工业品纯度高,主要用于一般化学实验,不能用于分析工作,常以 LR表示。
以上按试剂纯度的分类法已在我国通用。根据化学工业部颁布的“化学试剂包装及标志”的规定,化学试剂的不同等级分别用各种不同的颜色来标志,见表1。
表1 我国化学试剂的等级及标志
bhclna2so4nano3na2co3
chclnaohna2co3nacl
dba(oh)2nahco3alcl3nahso4
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