| Bioactivity | 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]. |
| Target | EC50: 3 nM (β3-adrenoceptor) |
| Invitro | 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]. Animal Model: |
| Name | CL 316243 |
| CAS | 138908-40-4 |
| Formula | C20H18ClNNa2O7 |
| Molar Mass | 465.79 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 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 ag [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. |
CL 316243
CAS: 138908-40-4 F: C20H18ClNNa2O7 W: 465.79
CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2-
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