Cellagentech/Alcaftadine | Histamine (H1/H4) receptor antagonist/C25225/5 mg (powder)相关交流-蚂蚁淘在线

Cellagentech/Alcaftadine | Histamine (H1/H4) receptor antagonist/C25225/5 mg (powder)

苏州蚂蚁淘 /发布时间:1632160804 /浏览量:18

ProductDescription

Alcaftadine,aimidazobenzazepine-basedantagonistofthehistaminereceptors,hasapKiof8.5and5.8fortheH1receptorandH4receptors,respectively.Additionally,AlcaftadineshowshigheraffinityfortheH2receptorthanketotifen.[1]

Insupportofitspotentanti-inflammatoryproperties,Alcaftadinealsoexhibitsmodulatoryactiononimmunecellrecruitmentandmastcellstabilizingeffects.[2]Receptorbindingstudiesrevealedlesssignificanteffectsrangingfromamoderateaffinityforcholinergicmuscarinicreceptorsandloweraffinityforhumana2A-adrenoreceptors,serotonin5-H51A,5-HT2Areceptors,andmelanocortinMC4receptors.[2]Furthermore,displacementexperimentsshowedthatatconcentrationsupto10uM,Alcaftadinedidnotinteractwithotherreceptors,transporters,orionchannelbindingsites,includingthehERGchannel.[3]

Technicalinformation:

ChemicalFormula:		C₁₉H₂₁N₃O
CAS#:		147084-10-4
MolecularWeight:		307.38
Purity:		>98%
Appearance:		White
ChemicalName:		2-(1-Methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3,5,10,12-pentaene-6-carbaldehyde
Solubility:		Upto20mMinDMSO
Synonyms:		Alcaftadine,147084-10-4,Lastacaft

ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4^oCdesiccated,orstoreDMSOsolutionat-20^oC.

Reference:

1.	Gallois-Bernoisetal.,Alcaftadine,anewantihistaminewithcombinedantagonistactivityathistamineH1,H2,andH4receptors.J.ReceptorLigandChannelRes.2012,5,9-20.
2.	Namdaretal.,Alcaftadine:Atopicalantihistamineforuseinallergicconjunctivitis.DrugsofToday,2011,47(12),883-890.PubmedID:22348913
3.	Bohetsetal.,ClinicalPharmacologyofAlcaftadine,aNovelAntihistamineforthePreventionofAllergicConjunctivitis.J.Ocular.Pharm.Ther.2011,27(2),187-195.

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