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Xcessbio/AA92593, Antagonist of Melanopsin-mediated Photo-transduction-Xcessbio Biosciences Inc/5 mg solid/M60143-5s
MolecularWeight: | 269.36 |
Formula: | C13H19NO3S |
Purity: | ≥98% |
CAS#: | 457961-34-1 |
Solubility: | DMSOupto100mM |
ChemicalName: | 1-((4-methoxy-3-methylphenyl)sulfonyl)piperidine |
Storage: | Powder:4oC1year.DMSO:4oC3month;-20oC1year. |
BIOLOGicalActivity:
AA92593isapotentandselectivesmallmoleculeantagoNISTofmelanopsin-mediatedphoto-transduction(IC50~160nM).Itinhibitsmelanopsin(opsinamides)bycompetingwithretinalbindingtomelanopsin,andinhibitsitsfunctionwithoutaffectingrod-andcone-mediatedresponses.InvivoadministrationofAA92593tomicespecificallyandreversIBLymodifiedmelanopsin-dependentlightresponses,includingthepupillarylightreflexandlightaversion.Melanopsin,expressedinasubsetofretinalganglioncells,mediatesbehavioraladaptationtoambientlightandothernon-image-formingphoticresponses.ThediscoveryofAA92593raisestheProspectoftherapeuticcontrolofthemelanopsinphoto-transductionsystemtoregulatelight-dependentbehaviorandremediatepathologicalconditions.
HowtoUse:
Invitro:AA92593wasusedat10µMfinalconcentrationinvariousinvitroassays.
Invivo:AA92593wasdosedintraperitoneally30mg/kg20minbeforePLRmeasurementattenuatedpupilconstrictioninresponsetolight(1013phcm-2s-1)by~50%inadultrdmice.
Reference:
- 1.JonesKA,etal.Small-moleculeantagonistsofmelanopsin-mediatedphototransduction.(2013)NatChemBiol.9(10):630-5.