BRL 37344 (sodium salt)

BRL 37344 (sodium salt)CAS号: 127299-93-8分子式: C19H21ClNO4·Na分子量: 385.82描述纯度储存/保存方法形态别名外观PK值Ki 数据可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

BRL 37344, sodium salt is a potent and selective agonist of β3 adrenoceptor with Ki values of 287, 1750 and 1120 nM for β3, β1 and β2 receptors, respectively .

纯度
98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
形态
Solid
基本信息
别名
BRL 37344 Na Salt
外观
white powder
PK值
pKa: 3.18 (Predicted), pKb: 8.98 (Predicted)
Ki 数据
β3 receptor: Ki= 287 nM; β1 receptor: Ki= 1750 nM; β2 receptor: Ki= 1120 nM
可溶性/溶解性
Soluble in water (100 mM).
生物活性
靶点
β3 receptor
In vitro(体外研究)
BRL 37344, sodium salt is a potent and selective β3 adrenoceptor agonist. In isolated rat brown and white adipocytes, BRL 37344 significantly stimulated lipolysis with EC50 values of 5 and 56 nM in brown adipocytes and white adipocytes, respectively. In the isolated guinea pig heart, BRL 37344 (10-8-10-5 M) increased heart contractility (dP/dt) and coronary flow (CF). However, BRL 37344 (10-8 M) completely inhibited isoprenaline-induced increase in contractility, which suggested that BRL 37344 display β1-antagonistic properties.
In vivo(体内研究)
In fasted rabbits, BRL 37344 significantly increased plasma nonesterified fatty acids (NEFA) levels through β3-adrenoceptor. However, BRL 37344 had no effect on plasma glucose levels. In mice, BRL 37344 increased circulating transaminase levels through activation of β3-adrenoceptor.

分子结构图

BRL 37344 (sodium salt)