KR-33493-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKR-33493Cat.No.:HY-100755CASNo.:1021497-97-1分?式:C??H??BrN?O?S分?量:460.34作?靶點(diǎn):TNFReceptor作?通路:Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:≥31mg/mL(67.34mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1723mL10.8615mL21.7231mL5mM0.4345mL2.1723mL4.3446mL10mM0.2172mL1.0862mL2.1723mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.43mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.43mM);ClearsolutionBIOLOGICALACTIVITY?物活性KR-33493?個(gè)有效的Fas介導(dǎo)細(xì)胞死亡(FAF1)的抑制劑。IC50&TargetFas體內(nèi)研究BodyweightchangesofbothsexesarenotrelatedtoKR-33493inalldoses.InratsadministratedKR-33493for4weeks,notestarticle-relatedchangesinanytreatedgroupsofeithersexarefoundinhematology,serumbiochemistry,andurinalysis.IndogsadministratedKR-33493for2weeks,redbloodcellcount(RBC)valueinmalesissignificantlyhigheratthe1000mg/kg/daydosethanthatofthecontrolgroup(i.e.,6.96±0.323vs.6.12±0.418).However,thechangeofRBCisrecoveredaftertheendoftheadministrationperiod.Thedose-normalizedAUClastisnotsignificantlydifferentbetweenthegroups,suggestingthatKR-33493isgovernedbylinearkinetics[1].PROTOCOLAnimalAtotalof93maleand93femalespecificpathogen-freerats(6weeksofage),and16maleand16femaleAdministration[1]beagledogs(8monthsofage)areusedinthisstudy.Inatoxicokineticstudy,ratbloodsamples(approximately0.6mL)arecollectedintotubescontainingheparinfromthelateraltailveinat0,0.5,1,2,4,8,12,and24hafterdosingwithKR-33493atdosesof50,150,and500mg/kg/dayonDay1andWeek4.Dogbloodsamples(approximately0.6mL)arecollectedintotubescontainingEDTA-2Kfromthecephalicveinat0,0.5,1,2,4,6,8,and24hafterdosingatKR-33493dosesof50,250,and1000mg/kg/dayonDay1andWeek2.Theplasmaisseparatedbycentrifugation(approximately132,000g,3min,4°C)andstoredatapproximately-80°Cuntilanalysis.TheKR-33493concentrationinplasmaisquantified[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].JeongJW,etal.SubacutetoxicityevaluationofKR-33493,FAF1inhibitorforanewanti-parkinson'sdiseaseagent,afteroraladministrationinratsanddogs.RegulToxicolPharmacol.2016Nov;81:387-396.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo