产品描述

Pitolisant hydrochloride is a potent and selective inverse agonist of the histamine H3 receptor(Ki : 0.16 nM).

靶点活性

H3 receptor,0.16 nM(ki)

体外活性

体内活性

Mice fed with high-fat diet showed more weight gain throughout the 12-week period of inducing obesity. Animals fed with high-fat diet and treated with pitolisant (next 14 days) showed significantly less weight gain than mice from the control group consuming a high-fat diet. From the 10th day of the pitolisant administration, a statistically significant difference in body weight between the groups was observed. Metformin, which served as a positive control, reduced body weight from the ninth day of administration onward[1].

动物实验

Male CD-1 mice were fed on high-fat diet consisting of 40% fat blend (Labofeed B with 40% lard) for 14 weeks, water and 30% sucrose available ad libitum. Control mice were fed on a standard diet and drank water only. After 12 weeks, mice with obesity induced via their diet were randomly divided into three equal groups that had the same mean body weight and were treated intraperitoneally with test compounds at the following doses: pitolisant 10 mg/kg bw/day or metformin 100 mg/kg bw/day; control group: vehicle =1% Tween 80, 0.35 ml/kg (high-fat/sugar diet + vehicle = obesity control group) once daily in the morning, between 9:00 and 10:00 AM for 14 days. Control mice (control without obesity) were maintained on a standard diet, with intraperitoneal administration of vehicle = 1% Tween 80, 0.35 ml/kg (standard diet + vehicle = control group). Water and sucrose were measured daily, immediately prior to administration of drugs. Animals always had free access to feed, water and sucrose[1].

分子量

332.31

分子式

C17H27Cl2NO

CAS

903576-44-3

溶解度

DMSO: 43 mg/mL (129.40 mM)

（ < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.