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Description | RapamycinisaspecificmTORinhibitorwithIC50of0.1nM. |
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IC50&Target | IC50:0.1nM(mTOR)[1] |
InVitro | RapamycininhibitsendogenousmTORactivityinHEK293cellswithIC50of0.1nM,morepotentlythaniRapandAP21967withIC50of5nMand10nM,respectively[1].RapamycinexertsitsantitumoreffectonmalignantgliomacellsbyinducingautophagyandsuggestthatinmalignantgliomacellsadisruptionofthePI3K/AktsignalingpathwaycouldgreatlyenhancetheeffectivenessofmTORinhibitors.RapamycininhibitscellviABIlityinallthreecelllinesinadose-dependentmanner,buttheirsensitivitiesvaried.TheIC50levelsofT98G,U87-MG,andU373-MGcellsare2nM,1μM,and>25μM,respectively[3]. |
InVivo | TreatmentwithRapamycin(i.p,1.5mg/kg)almostcompletelypreventsthehypertrophicincreasesinplantarismuscleweightandfibresizeat7and14days[4].WTorLS/+micearetreateddailyRapamycin(2mg/kgbodyweighti.p.)for4weeks,followsbyanadditional4weeksofweeklyinjectionsofthesamedose.ThereissignificantreversaloftheabnormalfetalgeneexpressionprofileofheartsfromRapamycin-treatedLS/+mice[5]. |
ClinicalTrial | ViewMoreCollapse |
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PreparingStockSolutions |
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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KinaseAssay [1] | HEK293cellsareplatedat2-2.5×105cellsperwellofa12-wellplateandserum-starvedfor24hinDMEMonly.Cellsaremock-treatedortreatedwithRapamycin(0.05-50nM),iRap(0.5-500nM),orAP21967(0.5-500nM)for15minutesat37°C.Serumisaddedtoafinalconcentrationof20%for30minutesat37°C.CellsarelysedandcelllysatesareseparatedbySDS-PAGE.ResolvedproteinsaretransferredtoaPVDFmembraneandimmunoblottedwithaphosphospecificprimaryantibodyagainstThr389ofp70S6kinase.DataareanalyzedusingImageQuantandKaleidaGraph[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
CellAssay [2] | RapamycinisdissolvedinDMSOandstored,andthendilutedwithappropriatemediumbeforeuse[2]. HL-60,NB4,U937,KG-1,andK562cellsarepassagedroutinelyinRPMI-1640supplementedwith10%heat-inactivatedFBS,2mML-glutamine,50U/mLpenicillinand50μg/mLstreptomycinina5%CO2humidifiedatmosphereat37°C.Fortheexperiments,exponentiallygrowingcellsareharvestedbycentrifugation,andresUSPendedinfreshmediumcontaining10%FBS.Thecellsareseededataninitialcelldensityof2×105/mLinBDFalconsix-wellplatesinthepresenceofvariousconcentrationsofDMSOor1μMATRA.Rapamycin(20nM)isadded20minpriortothedifferentiationagents.Atday2,0.3mLoffreshmediumisaddedtoeachwell.Theviablecellsaredeterminedbytrypanblueexclusionandquantifiedusingahemocytometer[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly. | ||||||||||||||||
AnimalAdmiNISTration [4][5] | Rapamycinisdissolvedin2%carboxymethylcellulose(Rat)[4]. Rat[4] | ||||||||||||||||
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MolecularWeight | 914.17 | ||||||||||||
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Formula | C₅₁H₇₉NO₁₃ | ||||||||||||
CASNo. | 53123-88-9 | ||||||||||||
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Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
Solvent&Solubility | DMSO:≥28mg/mL Rapamycinispreparedinvehicle(16%DMSOin0.5w/v%methylcellulose400)[6]. *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">1> | ||||||||||||
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Purity:98.98%
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如题,之前没做过药代,老师给了一个600+Da的五肽,想测下药代动参数,看文献推荐上述两种方法,但是不知道选哪种更好,lcms前处理会不会影响小肽。
求助大家,小分子药物最新专利申请情况跟踪,之前听别人说可以在一个网站可以导出这个信息。
不知哪位大侠知道,告知一下,不胜感激!
westblot蛋白免疫印迹实验跑小分子蛋白(15kd)条带一直是波浪状,有人说是胶的问题,可同时跑了36kd蛋白,条带是直的,有人说是要恒流跑,电压不要太大,我的转膜条件是50v,50min,请教各位大神指点,万分感谢!!!
求助各位前辈,我最近在合成的化合物水溶性很好,非常好,以至于可以随便溶解在水里,它的六氟磷酸盐也可以随意溶解在水里(大于50uM),细胞成像实验显示它根本进不去细胞,求问有没有啥方法包裹一下让它进去?我搜了一下文献,感觉多数是把脂溶性特别好的东西包裹一下弄进去的,也许是搜索姿势不对没找到我需要的答案,**点拨啊!!!
一、首先你要明白肽是什么...........................肽是氨基酸通过酰胺键结合而成的东西.........
二、你要明白氨基酸是什么..........................氨基酸是构成蛋白质的基本单位,多种氨基酸结合为长肽链,几条长肽链再盘旋就形成了蛋白质......................
三、关于小分子肽、短肽、多肽、寡肽.......其实都是肽.......区别只是由多少个氨基酸构成而已............
所以,你的问题可以很粗暴地理解为“蛋白质对人体有没有副作用”.......
如果你营养足够的情况下,再补充这个,会导致营养过剩,从而加重身体代谢的负荷............类似就是这样子的了...........小分子肽,一般现在用于化妆品上比较多(一ye子.植物肽面膜就是这个).......小分子肽(可以简单理解为纳米胶原蛋白),这比蛋白质(也可以粗暴理解为胶原蛋白)更加容易吸收......而用在食品上,要视乎是何种小分子肽了.....大豆肽、花生肽、大米肽....不同的肽有不同的功效.......主要可以改善风味、改善吸收、增强胃肠道功能等等.......
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