ProductDescription
VX-765isanorally-availableprodrugofVRT-043198,aninhibitorofinterleukin-convertingenzyme/caspase-1subfamilycaspases.VRT-043198showsKivaluesof0.8nMand100-foldselectivityoverothernon-ICEsubfamilycaspases.VRT-043198showednosignificantactivitytowardstrypsinorcathepsinB.(1)
VRT-043198inhibitsIL-1breleasefrombothPBMCsandwholebloodwithIC50valuesof0.67and1.9uM,respectively.AdditionallyinstimulatedPBMCs,VRT-043198dose-dependentlyinhibitedIL-1b,IL-18,andIFN-g,withoutaffectingTNF-arelease.Inahypoxia-inducedapoptosisassayemployingtheNT2humanneuroblastomacellline,VRT-043198didnotalterischemia-inducedapoptosisuptoconcentrationsof100uM.(1)
AccordingtoVertex"snewsrelease,VX-765hasbeenshowntoinhibitacuteseizuresinpreclinicalmodelsofacuteepilepsyandhasshownactivityinpreclinicalmodelsofchronicepilepsythatdonotrespondtostandardanti-epilepticdrugs.(2)
Technicalinformation:
| ChemicalFormula: | C24H33ClN4O6 | |
| CAS#: | 273404-37-8 | |
| MolecularWeight: | 509 | |
| Purity: | >98% | |
| Appearance: | white | |
| ChemicalName: | (S)-1-((S)-2-(4-amino-3-chlorobenzamido)-3,3-dimethylbutanoyl)-N-((2R,3S)-2-ethoxy-5-oxotetrahydrofuran-3-yl)pyrrolidine-2-carboxamide | |
| Solubility: | Upto50mMinDMSO | |
| Synonyms: | VX-765,VX765 |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Wannamakeretal.,(S)-1-((S)-2-{[1-(4-Amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylicacid((2R,3S)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide(VX-765),anOrallyAvailableSelectiveInterleukin(IL)-ConvertingEnzyme/Caspase-1Inhibitor,ExhibitsPotentAnti-InflammatoryActivitiesbyInhibitingtheReleaseofIL-1bandIL-18.J.Pharmacol.Exp.Ther.2007,321(2),509-516.PubmedID:17289835 |
| 2. | http://investors.vrtx.com/releasedetail.cfm?ReleaseID=555967 |
Cellagen的FlexiWash FW400自动膜/凝胶洗涤站设计用于自动Western blot膜洗涤和孵育过程。将蛋白质转移到膜上后，将膜加载到FlexiWash上以进行自动封闭，孵育和洗涤循环。用户只需要准备所需的试剂，启动印迹程序，然后让FW400进行其余操作即可。凭借独特的液体处理设计，FW400同时支持四个清洗/孵育过程，每个过程均可独立编程，并针对特定应用实现全自动。FW400也可用于蛋白质或DNA凝胶染色和脱色，或涉及重复液体处理和孵育周期的任何其他应用。
