Bioactivity | CL316243 free acid is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors. CL316243 free acid is a effective stimulant of adipocyte lipolysis and increases brown adipose tissue thermogenesis and metabolic rate. CL316243 free acid has the potential for the treatment obesity, diabetes and urge urinary incontinence[1][2][3]. |
Invitro | CL 316243 free acid 对大鼠心脏和大鼠比目鱼肌的 IC50 值分别为 0.6 μM 和 1 μM[1]。 CL 316243 free acid 抑制自发收缩,以浓度依赖性方式分离的大鼠逼尿肌条,平均浓度抑制 50% 的最大反应 2.65 nM[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CL 316243 free acid 相关抗体: |
In Vivo | CL316243 free acid (皮下注射;0.1 mg/kg/d;每天一次;1 周) 提高 BAT 中 UCP1 的 mRNA 和蛋白表达水平,与饮食无关[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 183720-02-7 |
Formula | C20H20ClNO7 |
Molar Mass | 421.83 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Bloom JD, et al. Disodium (R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino] propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent beta-adrenergic agonist virtually specific for beta 3 receptors. A promising antidiabetic and antiobesity agent.J Med Chem. 1992 Aug 7;35(16):3081-4. [2]. Shin W, et al. Impaired adrenergic agonist-dependent beige adipocyte induction in obese mice.J Vet Med Sci. 2019 Jun 6;81(6):799-807. [3]. Woods M, et al. Efficacy of the beta3-adrenergic receptor agonist CL-316243 on experimental bladder hyperreflexia and detrusor instability in the rat. J Urol. 2001 Sep;166(3):1142-7. |