JTE-607-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJTE-607Cat.No.:HY-110133CASNo.:188791-09-5分?式:C??H??Cl?N?O?分?量:597.36作?靶點(diǎn):Others作?通路:Others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:250mg/mL(418.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.6740mL8.3702mL16.7403mL5mM0.3348mL1.6740mL3.3481mL10mM0.1674mL0.8370mL1.6740mL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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)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%salineSolubility:≥2.08mg/mL(3.48mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.48mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.48mM);ClearsolutionBIOLOGICALACTIVITY?物活性JTE-607?種?選擇性的炎性細(xì)胞因?合成抑制劑，可保護(hù)??免受內(nèi)毒素休克。JTE-607作?于LPS刺激的?PBMC，抑制TNF-α、IL-1β、IL-6、IL-8和IL-10的IC50分別為11、5.9、8.8、7.3和9.1nM[1]。斷裂和聚腺苷酸化特異因?3(CPSF3)JTE-607的靶蛋?[2]。體外研究JTE-607inhibitsinflammatorycytokineproduction,includingTNF-α,IL-1β,IL-6,IL-8andIL-10,fromLPS-stimulatedhumanPBMCs,withIC50sof11,5.9,8.8,7.3and9.1nM,respectively.TheinhibitoryeffectsofJTE-607arealsoseeninmRNAexpressionofthosecytokines[1].JTE-607inhibitsinflammatorycytokineproductionfromLPS-stimulatedhumanPBMCswithanIC50ofapproximately10nM[1].JTE607inhibitsLPS-stimulatedIL-8productionfrommonkeyandrabbitPBMCs,andTNF-αproductionfrommouseandratPBMCswithIC50sof59,780,1600and19000nM,respectively[1].JTE607alsosuppressesothercytokines,granulocyte-macrophagecolonystimulatingfactorandIL-1RAwithIC50sof2.4±0.8and5.4±0.4nM,respectively[1].JTE-607inhibitscytokineproductioninmonkey,rabbit,mouseandratwithIC50sof59±26,780±120,1600±650and19000±3200nM,respectively[1].RT-PCR[1]CellLine:humanperipheralbloodmononuclearcells(PBMCs)Concentration:100nMIncubationTime:20hoursResult:ReducedtheincreaseinthelevelofmRNAsofTNF-α,IL-1b,IL-6andIL-8.體內(nèi)研究JTE-607(0.3-10mg/kg,i.v.)showsdosedependentinhibitionofmortalityafterLPSchallengeinC.parvumsensitizedmiceinaccordancewithadecreaseofplasmaTNF-α[1].AnimalModel:MaleC57BL/6mice(5to6weeksold)aresensitizedbyinjectingCorynebacteriumparvum[1]Dosage:0.3,1,3,10mg/kgAdministration:Administeredintravenously10minbeforetheLPSchallenge.Result:Showeddosedependentinhibitionofthemortalityat0.3to10mg/kgandsignificant2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEeffectat3and10mg/kg.REFERENCES[1].MKakutani,etal.JTE-607,anovelinflammatorycytokinesynthesisinhibitorwithoutimmunosuppression,protectsfromendotoxinshockinmice.InflammRes.1999Aug;48(8):461-8.[2].NathanTRoss,etal.CPSF3-dependentpre-mRNAprocessingasadruggablenodeinAMLandEwing'ssarcoma.NatChemBiol.2020Jan;16(1):50-59.McePdfHeightCaution:Producthasnotbeenfu