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Submit ReviewCL 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.
分子量 | 465.8 |
公式 | C20H18ClNNa2O7 |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 138908-40-4 |
PubChem ID | 5312115 |
InChI Key | FUZBPOHHSBDTJQ-CFOQQKEYSA-L |
Smiles | [Na+].[Na+].C[C@H](CC1=CC=C2OC(OC2=C1)(C([O-])=O)C([O-])=O)NC[C@H](O)C1=CC=CC(Cl)=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 46.58 | 100 |
以下数据基于产品分子量 465.8。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.15 mL | 10.73 mL | 21.47 mL |
5 mM | 0.43 mL | 2.15 mL | 4.29 mL |
10 mM | 0.21 mL | 1.07 mL | 2.15 mL |
50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
参考文献是支持产品生物活性的出版物。
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 a J.Med.Chem. 35 3081 PMID: 1354264
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
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关键词: CL 316243 disodium salt, CL 316243 disodium salt supplier, selective, β3-adrenoceptor, b3-adrenoceptor, β3-adrenergic, b3-adrenergic, agonists, Receptors, CL316243, disodium, salt, 151126-84-0, Adrenergic, Beta-3, 1499, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 CL 316243 disodium salt 的部分引用包括:
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
De-Lima-Junior et al (2019) Abnormal brown adipose tissue mitochondrial structure and function in IL10 deficiency. EBioMedicine 39 436 PMID: 30502051
Feng et al (2019) Identification of a rhodanine derivative BML-260 as a potent stimulator of UCP1 expression. Theranostics 9 3501 PMID: 31281493
Li (2017) An additive effect of promoting thermogenic gene expression in mice adipose-derived stromal vascular cells by combination of rosiglit. and CL316,243 Int J Mol Sci 18 E1002 PMID: 28481288
Blaszkiewicz et al (2019) Neuropathy and neural plasticity in the subcutaneous white adipose depot. PLoS One 14 e0221766 PMID: 31509546
Fischer et al (2017) A miR-327-FGF10-FGFR2-mediated autocrine signaling mechanism controls white fat browning. Nat Commun 8 2079 PMID: 29233981
Huang et al (2017) Transcription factor Hlx controls a systematic switch from white to brown fat through Prdm16-mediated co-activation. Nat Commun 8 68 PMID: 28701693
Gonzalez-Hurtado et al (2018) Fatty acid oxidation is required for active and quiescent brown adipose tissue maintenance and thermogenic programing. Mol Metab 7 45 PMID: 29175051
Kashyap et al (2015) Characterization of the role of HCN channels in β3-adrenoceptor mediated rat bladder relaxation. Cell Rep 2 PMID: 26709376
Patsouris et al (2015) Burn Induces Browning of the Subcutaneous White Adipose Tissue in Mice and Humans. Nat Commun 13 1538 PMID: 26586436
Berbée et al (2015) Brown fat activation reduces hypercholesterolaemia and protects from atherosclerosis development. J Neurosci 6 6356 PMID: 25754609
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
Saxton et al (2018) Role of Sympathetic Nerves and Adipocyte Catecholamine Uptake in the Vasorelaxant Function of Perivascular Adipose Tissue. Arterioscler Thromb Vasc Biol 38 880 PMID: 29496660
Chen et al (2016) Exosomal microRNA miR-92a concentration in serum reflects human brown fat activity. Bladder (San Franc) 7 11420 PMID: 27117818
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
Chen et al (2018) Cbx4 Sumoylates Prdm16 to Regulate Adipose Tissue Thermogenesis. Cell Rep 22 2860 PMID: 29539416
Masand et al (2018) Proteome Imbalance of Mitochondrial Electron Transport Chain in Brown Adipocytes Leads to Metabolic Benefits. Cell Metab 27 616 PMID: 29514069
Mössenböck et al (2014) Browning of white adipose tissue uncouples glucose uptake from Ins signaling. PLoS One 9 e110428 PMID: 25313899
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
Pan et al (2014) MicroRNA-378 controls classical brown fat expansion to counteract obesity. Nat Commun 5 4725 PMID: 25145289
Nackley et al (2007) Catechol-O-methyltransferase inhibition increases pain sensitivity through activation of both beta2- and beta3-adrenergic receptors. Pain 128 199 PMID: 17084978
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.