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MedChemExpress - Model CL 316243 - ...

MedChemExpress - Model CL 316243 - 138908-40-4

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].

CL 316243

MCE China：CL 316243

Brand：MedChemExpress (MCE)

Cat. No.HY-116771A

CAS：138908-40-4

Purity：99.98%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：CL316243 is a highly potent selective β3-adrenoceptor agonist with a EC50 of 3 nM, but is an extremely poor to β1/2- receptors.CL316243 is a 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.

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].

IC50 & Target：β adrenergic receptor

References：

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Brand introduction:
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•   The biological activity of the products has been verified by the experiments of customers in various countries；
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