您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > 5HT6-ligand-1
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
5HT6-ligand-1
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。
5HT6-ligand-1图片
CAS NO:1038988-11-2
包装:5 mg
市场价:7000元

产品介绍

产品描述

5HT6-ligand-1 is a potent 5-HT6 receptor ligand (Ki: 1.43 nM).

体内活性

5HT6-ligand-1 is extensively metabolized in rat liver microsomes whereas in human liver microsomes, 5HT6-ligand-1 is extensively metabolized (90%). The IC50 values for 5HT6-ligand-1 at CYP 3A4 is 35.97%, whereas the IC50 values at CYP 2D6 enzymes are less than 20 μM. 5HT6-ligand-1 at an oral dose of 10 mg/kg is rapidly absorbed in rats with a good oral half-life of 3.17±0.49 h with an oral bioavailability of 29±5%. The observed oral Cmax is 60±44 ng/mL and occurs at 1.83 h. 5HT6-ligand-1 displays an oral exposure of 217±92 ng h/mL. It has a clearance of 220±92 mL/min/kg with a volume of distribution of 32.6±10.7 L/kg for iv dose. Extensive rat metabolism coupled with high clearance could be the possible reason for moderate oral bioavailability showed by 5HT6-ligand-1. Oral administration of 5HT6-ligand-1 reverses the time delay induced memory deficit and a statistically significant effect is observed at a dose of 10 mg/kg indicating cognitive improvement potential of the compound 6a.

Cas No.

1038988-11-2

分子式

C20H22BrN3O2S

分子量

448.38

别名

5HT6-ligand-1

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years