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Idalopirdine Hydrochloride
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。
Idalopirdine Hydrochloride图片
CAS NO:467458-02-2
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
Lu AE58054 Hydrochloride
Lu AE58054盐酸盐
Idalopirdine HCl
产品介绍
Idalopirdine Hydrochloride 是一种选择性的5-HT6 受体拮抗剂,Ki为 0.83 nM。

产品描述

Lu AE58054 hydrochloride is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist (Ki: 0.83 nM).

体外活性

In the 5-HT(6) GTP gamma S efficacy assay, Lu AE58054 showed potent inhibition of 5-HT-mediated activation. Apart from medium affinity to adrenergic alpha (1B)- and alpha(1A)-adrenoreceptors, Lu AE58054 shows >50-fold selectivity compared with more than 70 targets examined[1].

体内活性

In the rats model, Orally administered Lu AE58054 inhibited binding of the 5-HT6 antagonist Lu AE60157 (ED50: 2.7 mg/kg). Administration of Lu AE58054 in a dose range (5–20 mg/kg) leading to above 65% 5-HT6R binding, which reversed cognitive impairment in rats treatment with phencyclidine. These results indicate that Lu AE58054 is a potent antagonist of 5-HT6Rs with good oral bioavailability in the rat model of cognitive impairment in schizophrenia[1].

Cas No.

467458-02-2

分子式

C20H20ClF5N2O

分子量

434.83

别名

Lu AE58054 Hydrochloride;Lu AE58054盐酸盐;Idalopirdine HCl

储存和溶解度

H2O:3 mg/mL(6.90 mM, with ultrasonic and warming),with ultrasonic and warming
DMSO:20 mg/mL(45.99 mM)
Ethanol:50 mg/mL(114.99 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years