H3B-120-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEH3B-120Cat.No.:HY-136128CASNo.:2194903-42-7分?式:C??H??N?O?S分?量:372.48作?靶點:PotassiumChannel作?通路:MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:62.5mg/mL(167.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6847mL13.4235mL26.8471mL5mM0.5369mL2.6847mL5.3694mL10mM0.2685mL1.3424mL2.6847mL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，并請注意儲備液的保存?式和期限。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.58mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.58mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.58mM);Clearsolution1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性H3B-120?種?選擇性，競爭性和變構的氨甲酰磷酸合成酶1(CPS1)抑制劑，IC50為1.5μM，Ki為1.4μM。H3B-120具有抗癌活性。IC50&TargetIC50:1.5μM(CPS1)[1]Ki:1.4μM(CPS1)[1]體外研究H3B-120hasnoinhibitionofCPS2activityofCAD(CPS2,aspartyltranscarbamylase,dihydroorotase)[1].H3B-120achievesinhibitionbybindingtoanallostericpocketsituatedbetweentheintegratingandATPAdomains[1].H3B-120(25,50,75,100μM)inhibitsureaproductioninadose-dependentmanner,althoughthecellularpotencydecreasessignificantlycomparedwithenzymaticassays[1].Thehalf-lifeofH3B-120isonly40min[1].REFERENCES[1].YaoS,etal.SmallMoleculeInhibitionofCPS1ActivitythroughanAllostericPocket.CellChemBiol.2020Mar19;27(3):259-268.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-