LC Labs/C1502 Celecoxib, >99%/C1502/25 g

• CelecoxibisahighlyselectiveCOX-2inhibitorandprimarilyinhibitsprostaglandinproduction.
• Celecoxibisapproximately7.6-foldmoreselectiveforCOX-2inhibitionoverCOX-1.Thisspecificityallowscelecoxibtoreduceinflammationandpainwhileminimizinggastrointestinaladversedrugreactions(e.g.stomachulcers)thatarecommonwithnon-selectivenon-steroidalanti-inflammatorydrugs(NSAIDs).Silverstein,F.E.,etal."Gastrointestinaltoxicitywithcelecoxibvsnonsteroidalanti-inflammatorydrugsforosteoarthritisandrheumatoidarthritis:theCLASSstudy:Arandomizedcontrolledtrial.CelecoxibLong-termArthritisSafetyStudy."JAMA.284:1247-1255(2000).
• CelecoxibandotherCOX-2inhibitorsincreasetheriskofmyocardialinfarction.Caldwell,B.,etal."Riskofcardiovasculareventsandcelecoxib:asystematicreviewandmeta-analysis."J.R.Soc.Med.99:132-140(2006).
• COX-2notonlyplaysanimportantroleininflammationbutalsoisinvolvedinmultiplebiologiceventsthroughoutthetumorigenicprocess.COX-2inhibitorsmayactadditivelyorsynergisticallywithcurrentlyusedcytotoxicsandmolecularlytargetedagentstopreventandtreatcancers.Koki,A.T.andMasferrer,J.L."Celecoxib:aspecificCOX-2inhibitorwithanticancerproperties."CancerControl.9:28-35(2002).
• CelecoxibshowscompetitivekineticsonCOX-1(Ki=10-16µM).ItalsodisplaysaninitialcompetitiveinteractionwithCOX-2(Ki=11-15µM),followedbyatime-dependentinteractionleadingtopotentinhibitionandinactivation(Kinact=0.03-0.5s-1).Half-maximalinhibition(IC50)usingend-pointassaysdemonstratesthecompetitivecomponentonCOX-1(IC50=4-19µM)andtheinactivationcomponentonCOX-2(IC50=0.003-0.006µM).Gierse,J.K.,etal."Kineticbasisforselectiveinhibitionofcyclo-oxygenases."BiochemJ.339:607-614(1999).
• CelecoxibistheactiveingredientinthedrugsoldunderthetradenameCelebrex®orCelebra®insomecountries.Ithasbeenapprovedinatleastonecountryfortreatmentofpatientswithosteoarthritis,rheumatoidarthritis,acutepain,painfulmenstruationandmenstrualsymptoms,anditisalsousedtoreducenumbersofcolonandrectumpolypsinpatientswithfamilialadenomatouspolyposis.NOTE:ThecelecoxibsoldbyLCLaboratoriesisNOTCelebrex®orCelebra®,andisNOTforhumanuse.
• Soldforlaboratoryormanufacturingpurposesonly;notforhuman,medical,veterinary,food,orhouseholduse.
• ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanadianpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
• Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.

RelatedTerms:

[Celebrex][Celebra][Celecox][Onsenal][Solexa][SC-58635][YM-177]
M.W.381.37
C17H14F3N3O2S
[169590-42-5]
M.I.14:1956

Storage

Storeatorbelow-20ºC

Solubility

SolubleinDMSOat200mg/mL;solubleinethanolat100mg/mL;verypoorlysolubleinwater;maximumsolubilityinplainwaterisestimatedtobeabout10-50µM;buffers,serum,orotheradditivesmayincreaseordecreasetheaqueoussolubility

Disposal

A