CL 316243 disodium salt

Cat. No. 1499

CL 316243 disodium salt C20H18ClNNa2O7 [151126-84-0]

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Chemical Name: 5-[(2R)-2-[[(2R)-2-(3-Chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,2-dicarboxylic acid disodium salt

Biological Activity

Potent and highly selective β3-adrenoceptor agonist (EC50 = 3 nM); > 10000-fold selective over β1 and β2 receptors. Increases brown adipose tissue thermogenesis and metabolic rate, and decreases blood insulin and glucose levels following oral administration in vivo.

Technical Data

M.Wt:
465.8
Formula:
C20H18ClNNa2O7
Solubility:
Soluble to 100 mM in water
Purity:
>98 %
Storage:
Desiccate at -20°C
CAS No:
151126-84-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Woods et al (2001) Efficacy of the β3-adrenergic receptor agonist CL-316243 on experimental bladder hyperflexia and detrusor instability in the rat. J.Urol. 166 1142. PMID: 11490313.

Yoshida et al (1994) Anti-obesity and anti-diabetic effects of CL 316,243, a highly specific β3-adrenoceptor agonist, in yellow KK mice. Life Sci. 54 491. PMID: 8309351.

Bloom et al (1992) Disodium(R,R)-5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]-amino]propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL 316,243). A potent β-adrenergic agonist virtually specific for β3 receptors. A promising antidiabetic and antiobesity agent. J.Med.Chem. 35 3081. PMID: 1354264.

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Citations are publications that use Tocris products. Selected citations for CL 316243 disodium salt include:

Chen et al (2016) Exosomal microRNA miR-92a concentration in serum reflects human brown fat activity. Bladder (San Franc) 7 11420. PMID: 27117818.

Berbée et al (2015) Brown fat activation reduces hypercholesterolaemia and protects from atherosclerosis development. J Neurosci 6 6356. PMID: 25754609.

Kashyap et al (2015) Characterization of the role of HCN channels in β3-adrenoceptor mediated rat bladder relaxation. Cell Rep 2. PMID: 26709376.

Nagai et al (2015) Pulmonary Macrophages Attenuate Hypoxic Pulmonary Vasoconstriction via β3AR/iNOS Pathway in Rats Exposed to Chronic Intermittent Hypoxia. PLoS One 10 e0131923. PMID: 26132492.

Patsouris et al (2015) Burn Induces Browning of the Subcutaneous White Adipose Tissue in Mice and Humans. Nat Commun 13 1538. PMID: 26586436.

Mössenböck et al (2014) Browning of white adipose tissue uncouples glucose uptake from insulin signaling. PLoS One 9 e110428. PMID: 25313899.

Pan et al (2014) MicroRNA-378 controls classical brown fat expansion to counteract obesity. Nat Commun 5 4725. PMID: 25145289.

Suárez et al (2014) Oleoylethanolamide enhances β-adrenergic-mediated thermogenesis and white-to-brown adipocyte phenotype in epididymal white adipose tissue in rat. Dis Model Mech 7 129. PMID: 24159189.

Rieg et al (2012) Cardiovascular agents affect the tone of pulmonary arteries and veins in precision-cut lung slices. PLoS One 6 e29698. PMID: 22216346.

Enriori et al (2011) Leptin action in the dorsomedial hypothalamus increases sympathetic tone to brown adipose tissue in spite of systemic leptin resistance. Am J Pathol 31 12189. PMID: 21865462.

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