Sovesudil-PHP-201-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESovesudilCat.No.:HY-109191CASNo.:1333400-14-8Synonyms:PHP-201;AMA0076分?式:C??H??FN?O?分?量:407.44作?靶點(diǎn):ROCK作?通路:CellCycle/DNADamage;Cytoskeleton;StemCell/Wnt;TGF-beta/Smad儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(245.43mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4543mL12.2717mL24.5435mL5mM0.4909mL2.4543mL4.9087mL10mM0.2454mL1.2272mL2.4543mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.14mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.14mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.14mM);ClearsolutionBIOLOGICALACTIVITY?物活性Sovesudil(PHP-201)?種有效的、ATP競爭性局部作?Rho激酶(ROCK)抑制劑，對ROCKI和ROCKII的IC50分別為3.7和2.3nM。Sovesudil降低眼壓?不引起充?。IC50&TargetROCK-IROCK-II3.7nM(IC50)2.3nM(IC50)體外研究Sovesudil(PHP-201)(1μM;60min)isabletoinducealteredcellularbehaviorofhumantrabecularmeshwork(HTM)cells[1].體內(nèi)研究Sovesudil(0.1%,0.3%,and0.5%;maleNewZealandWhiterabbits)effectivelyreducesIntraocularPressure(IOP)inocularnormotensiveandacutehypertensiverabbitswithoutcausingdistincthyperemia[1].REFERENCES[1].VandeVeldeS,etal.AMA0076,anovel,locallyactingRhokinaseinhibitor,potentlylowersintraocularpressureinNewZealandwhiterabbitswithminimalhyperemia.InvestOphthalmolVisSci.2014;55(2):1006-1016.Published2014Feb18.[2].HaA,etal.Sovesudil(locallyactingrhokinaseinhibitor)forthetreatmentofnormal-tensionglaucoma:therandomizedphaseIIstudy[publishedonlineaheadofprint,2021Jul28].ActaOphthalmol.2021;10.1111/aos.14949.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchus