CL316243 是一种高效的 β3 肾上腺素受体选择性激动剂,EC50 为 3 nM。它是一种有效的脂肪细胞脂解刺激剂,可增加棕色脂肪组织的产热和代谢率,具有治疗肥胖症、糖尿病和急迫性尿失禁的潜力。
产品描述
CL316243 is a highly potent selective agonist of β3-adrenoceptor, with a EC50 of 3 nM. CL316243 is an effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence.
体外活性
CL 316243 displays binding affinities with IC50 values of 1 μM and 0.6 μM for rat soleus muscle and rat heart respectively. CL 316243 inhibits spontaneously contracting, isolated rat detrusor strips in a concentration-dependent manner with a mean concentration inhibiting 50% of the maximal response of 2.65 nM [1].
体内活性
CL316243 disodium (subcutaneously injection; 0.1 mg/kg/day; once a day; 1 week) elevates the mRNA and protein expression levels of BAT in UCP1 [2].
Cas No.
138908-40-4
分子式
C20H18ClNNa2O7
分子量
465.79
别名
CL 316243
储存和溶解度
H2O:80 mg/mL (171.75 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years