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Lu AE58054(Idalopirdine)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lu AE58054(Idalopirdine)图片
CAS NO:467459-31-0
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 398.37
FormulaC20H19F5N2O
CAS No. 467459-31-0;
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>10 mM in DMSO
Water: <1 mg/mL
Ethanol:
SMILES CodeFC1=CC(NC=C2CCNCC3=CC(OCC(F)(C(F)F)F)=CC=C3)=C2C=C1
SynonymsLu AE58054, Idalopirdine)
实验参考方法
In Vitro

In vitro activity: Orally administered Lu AE58054 potently inhibited striatal in-vivo binding of the 5-HT(6) antagonist radioligand [(3)H]Lu AE60157, with an ED(50) of 2.7 mg/kg. Steady-state modelling of an acute pharmacokinetic/5-HT(6)R occupancy time-course experiment indicated a plasma EC(50) value of 20 ng/ml.


Kinase Assay:


Cell Assay:

In VivoAdministration of Lu AE58054 in a dose range (5-20 mg/kg p.o.) leading to above 65% striatal 5-HT(6)R binding occupancy in vivo, reversed cognitive impairment in a rat novel object recognition task induced after subchronic treatment for 7 d with phencyclidine (PCP 2 mg/kg b.i.d., i.p. for 7 d, followed by 7 d drug free). The results indicate that Lu AE58054 is a selective antagonist of 5-HT(6)Rs with good oral bioavailability and robust efficacy in a rat model of cognitive impairment in schizophrenia
Animal model Rat
Formulation & Dosage 5-20 mg/kg; p.o
References Int J Neuropsychopharmacol. 2010 Sep;13(8):1021-33.Eur J Pharmacol. 2012 Feb 15;676(1-3):6-11.