Home / Adrenergic beta-3 Receptor Agonists / CL 316243 disodium salt

CL 316243 disodium salt

Catalog #: 1499
21 Citations Datasheet / COA / SDS
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1499/10
1499/50
CL 316243 disodium salt | CAS No. 138908-40-4 | Adrenergic beta-3 Receptor Agonists
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Description: Highly selective β3 agonist

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

Purity: ≥97%

Product Details
Citations (21)
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Biological Activity

CL 316243 disodium salt is a 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:
≥97%
Storage:
Store at -20°C
CAS No:
138908-40-4

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

Background References

  1. MicroRNA-378 controls classical brown fat expansion to counteract obesity.
    Pan, Dongning, Mao, Chunxiao, Quattrochi, Brian, Friedline, Randall, Zhu, Lihua J, Jung, Dae Youn, Kim, Jason K, Lewis, Brian, Wang, Yong-Xu
    Nat Commun, 2014;5(0):4725.
  2. Ablation of calcineurin Abeta reveals hyperlipidemia and signaling cross-talks with phosphodiesterases.
    Suk H, Zhou C, Yang T, Zhu H, Yu R, Olabisi O, Yang X, Brancho D, Kim J, Scherer P, Frank P, Lisanti M, Calvert J, Lefer D, Molkentin J, Ghigo A, Hirsch E, Jin J, Chow C
    J Biol Chem, 2013;288(5):3477-88.
  3. Transcription factor Hlx controls a systematic switch from white to brown fat through Prdm16-mediated co-activation
    L Huang, D Pan, Q Chen, LJ Zhu, J Ou, M Wabitsch, YX Wang
    Nat Commun, 2017;8(1):68.
  4. FABP3 and brown adipocyte-characteristic mitochondrial fatty acid oxidation enzymes are induced in beige cells in a different pathway from UCP1.
    Nakamura Y, Sato T, Shiimura Y, Miura Y, Kojima M
    Biochem Biophys Res Commun, 2013;441(1):42-6.
  5. Efficacy of the β3-adrenergic receptor agonist CL-316243 on experimental bladder hyperflexia and detrusor instability in the rat.
    Woods et al.
    J.Urol., 2001;166:1142
  6. Anti-obesity and anti-diabetic effects of CL 316,243, a highly specific β3-adrenoceptor agonist, in yellow KK mice.
    Yoshida et al.
    Life Sci., 1994;54:491
  7. 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 a
    Bloom et al.
    J.Med.Chem., 1992;35:3081

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Citations for CL 316243 disodium salt

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

21 Citations: Showing 1 - 10

  1. Identification of a rhodanine derivative BML-260 as a potent stimulator of UCP1 expression.
    Authors: Feng Et al.
    Theranostics  2019;9:3501
  2. Abnormal brown adipose tissue mitochondrial structure and function in IL10 deficiency.
    Authors: De-Lima-Junior Et al.
    EBioMedicine  2019;39:436
  3. Neuropathy and neural plasticity in the subcutaneous white adipose depot.
    Authors: Blaszkiewicz Et al.
    PLoS One  2019;14:e0221766
  4. Fatty acid oxidation is required for active and quiescent brown adipose tissue maintenance and thermogenic programing.
    Authors: Gonzalez-Hurtado Et al.
    Mol Metab  2018;7:45
  5. Role of Sympathetic Nerves and Adipocyte Catecholamine Uptake in the Vasorelaxant Function of Perivascular Adipose Tissue.
    Authors: Saxton Et al.
    Arterioscler Thromb Vasc Biol  2018;38:880
  6. Proteome Imbalance of Mitochondrial Electron Transport Chain in Brown Adipocytes Leads to Metabolic Benefits.
    Authors: Masand Et al.
    Cell Metab  2018;27:616
  7. Cbx4 Sumoylates Prdm16 to Regulate Adipose Tissue Thermogenesis.
    Authors: Chen Et al.
    Cell Rep  2018;22:2860
  8. Transcription factor Hlx controls a systematic switch from white to brown fat through Prdm16-mediated co-activation.
    Authors: Huang Et al.
    Nat Commun  2017;8:68
  9. A miR-327-FGF10-FGFR2-mediated autocrine signaling mechanism controls white fat browning.
    Authors: Fischer Et al.
    Nat Commun  2017;8:2079
  10. An additive effect of promoting thermogenic gene expression in mice adipose-derived stromal vascular cells by combination of rosiglit. and CL316,243
    Authors: Li
    Int J Mol Sci  2017;18(5):E1002
  11. Exosomal microRNA miR-92a concentration in serum reflects human brown fat activity.
    Authors: Chen Et al.
    Bladder (San Franc)  2016;7:11420
  12. Brown fat activation reduces hypercholesterolaemia and protects from atherosclerosis development.
    Authors: Berbée Et al.
    J Neurosci  2015;6:6356
  13. Characterization of the role of HCN channels in β3-adrenoceptor mediated rat bladder relaxation.
    Authors: Kashyap Et al.
    Cell Rep  2015;2
  14. Burn Induces Browning of the Subcutaneous White Adipose Tissue in Mice and Humans.
    Authors: Patsouris Et al.
    Nat Commun  2015;13:1538
  15. Pulmonary Macrophages Attenuate Hypoxic Pulmonary Vasoconstriction via β3AR/iNOS Pathway in Rats Exposed to Chronic Intermittent Hypoxia.
    Authors: Nagai Et al.
    PLoS One  2015;10:e0131923
  16. Browning of white adipose tissue uncouples glucose uptake from Ins signaling.
    Authors: Mössenböck Et al.
    PLoS One  2014;9:e110428
  17. Oleoylethanolamide enhances β-adrenergic-mediated thermogenesis and white-to-brown adipocyte phenotype in epididymal white adipose tissue in rat.
    Authors: Suárez Et al.
    Dis Model Mech  2014;7:129
  18. MicroRNA-378 controls classical brown fat expansion to counteract obesity.
    Authors: Pan Et al.
    Nat Commun  2014;5:4725
  19. Cardiovascular agents affect the tone of pulmonary arteries and veins in precision-cut lung slices.
    Authors: Rieg Et al.
    PLoS One  2012;6:e29698
  20. Leptin action in the dorsomedial hypothalamus increases sympathetic tone to brown adipose tissue in spite of systemic leptin resistance.
    Authors: Enriori Et al.
    Am J Pathol  2011;31:12189
  21. Catechol-O-methyltransferase inhibition increases pain sensitivity through activation of both beta2- and beta3-adrenergic receptors.
    Authors: Nackley Et al.
    Pain  2007;128:199

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