ProductDescription
MK0524,afusedindole-basedantagoNISTofprostaglandinD2(DP),hasaKibindingaffinityof0.57nMandaKddissociationconstantof0.03nM.WiththeexceptionoftheTxA2receptor(Ki=2.95nM),MK0524hasexcellentselectivityoveranumberofotherprostanoidreceptors(EPfamily,FP,andIP).Inafunctionalactivityassayinplatelet-richplasmaandwashedplatelets,MK0524hadanIC50of0.09nM.[1]
MK-0524hasbeenshowntoblocknicotinicacid-inducedcutaneousvasodilationandalsoantagonizesprostaglandinD1(DP1)inamouseDP1functionalassayatanIC50of1.1nM.[2]
Technicalinformation:
| ChemicalFormula: | C21H19ClFNO4S | |
| CAS#: | 571170-77-9 | |
| MolecularWeight: | 435.9 | |
| Purity: >98% | ||
| Appearance: | White | |
| ChemicalName: | [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-aceticacid | |
| Solubility: | Upto50mMinDMSO | |
| Synonyms: | MK-0524,MK-0524A,MK0524,Laropiprant,Cordaptive,Tredaptive |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Sturinoetal.,DiscoveryofaPotentandSelectiveProstaglandinD2ReceptorAntagonist,[(3R)-4-(4-Chlorobenzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-aceticAcid(MK-0524).J.Med.Chem.2007,50,794-806.PubmedID:17300164 |
| 2. | Chengetal.,AntagonismoftheprostaglandinD2receptor1suppressesnicotinicacid-inducedvasodilationinmiceandhumans.Proc.Natl.Acad.Sci.2006,103(17),6682-6687.PubmedID:16617107 |
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