Anamorelin hydrochloride；861998-00-7；Anamorelin HCl；anti CACS；anti NSCLC

Purity≥99%

white 

IntheFLIPRassay,Anamorelin(ANAM)showssignificantagonistactivityontheghrelinreceptor,withEC50valueof0.74nM.NosignificantantagonistactivityisobservedwithAnamorelinatconcentrationsofupto1,000nM.Inthebindingexperiments,Anamorelinbindstotheghrelinreceptorwithabindingaffinityconstant(Ki)of0.70nM.Inthecompetitionassaywithradiolabeledibutamoren(35S-MK-677;anotherghrelinreceptoragonist)Anamorelin(ANAM)isalsofoundtobindwChemicalbookithhighaffinitytotheghrelinreceptor(IC50=0.69nM).InratpituitarycellsincubatedwithAnamorelin,thereisadose-dependentstimulatoryeffectonGHreleaseandthepotency(EC50)is1.5nM.Anamorelinisscreenedforactivityagainstasetofover100receptors,ionchannels,transporters,andenzymes.Anamorelindemonstratesbindingtothetachykininneurokinin2(NK2)site(IC50=0.021μM);however,asubsequentNK2functionalassaydemonstratesnofunctionalactivity.

Inrats,Anamorelin(ANAM)atanoraldoseof3,10,or30mg/kgoncedailysignificantlyincreasesbothfoodintakeandbodyweightfromDay2toDay7oftreatmentcomparedwiththevehiclecontrol.ThecumulativechangeinfoodintakeandweightgainincreasChemicalbookesdose-dependently,andthesechangesaresignificantatalldoselevels(P<0.05)comparedtothecontrol.AdministrationofAnamorelinatasingleoraldoseof3,10,or30mg/kginducesadose-dependentincreaseinplasmaGHlevelsandGHAUC0-6hinrats.

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