CL 316243 NLT 98%

CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC₅₀ of 3 nM, but is an extremely poor to β1/2- receptors^[1].CL316243 is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate^[2]. CL316243 has the potential for the treatment obesity, diabetes and urge urinary incontinence^[3]. IC50 & Target: EC50: 3 nM (β3-adrenoceptor)^[1] In Vitro: CL 316243 displays binding affinities with IC₅₀ values of 0.6 μM and 1 μM for rat heart and rat soleus muscle respectively^[1].
CL 316243 inhibits spontaneously contracting, isolated rat detrusor strips in a concentration dependent manner with a mean concentration inhibiting 50% of maximal response of 2.65 nM^[3].
In Vivo: CL316243 disodium (subcutaneously injection; 0.1 mg/kg/day; once a day; 1 weeks) elevates the mRNA and protein expression levels of UCP1 in BAT, irrespective of diet^[2].