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Submit ReviewL-748,337 is a competitive β3-adrenoceptor antagonist that displays selectivity over β1 and β2 receptors (Ki values are 4.0, 204 and 390 nM for β3-, β2- and β1-adrenoceptors respectively). Inhibits cAMP accumulation in response to Isoproterenol (IC50 = 6 nM). Reduces iNOS expression, attenuates nitric oxide-induced cell proliferation and induces apoptosis in a melanoma cell line.
L-748,337 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 497.61 |
公式 | C26H31N3O5S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 244192-94-7 |
PubChem ID | 10028830 |
InChI Key | AWIONHVPTYTSHZ-DEOSSOPVSA-N |
Smiles | O[C@H](COC2=CC=CC(CNC(C)=O)=C2)CNCCC1=CC=C(NS(=O)(C3=CC=CC=C3)=O)C=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 | |||
DMSO | 49.76 | 100 | |
ethanol | 4.98 | 10 |
以下数据基于产品分子量 497.61。 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 | 2.01 mL | 10.05 mL | 20.1 mL |
5 mM | 0.4 mL | 2.01 mL | 4.02 mL |
10 mM | 0.2 mL | 1 mL | 2.01 mL |
50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
参考文献是支持产品生物活性的出版物。
Candelore et al (1999) Potent and selective human β3-adrenergic receptor antagonist. J.Pharmacol.Exp.Ther. 290 649 PMID: 10411574
Neidhold et al (2007) The function of α- and β-adrenoceptors of the saphenous artery in caveolin-1 knockout and wild-type mice. Br.J.Pharmacol. 150 261 PMID: 17179950
Dal Monte et al (2014) β3-adrenergic receptor activity modulates melanoma cell proliferation and survival through nitric oxide signaling. Naunyn Schmiedebergs Arch.Pharmacol. 387 533 PMID: 24599317
If you know of a relevant reference for L-748,337, please let us know.
关键词: L-748,337, L-748,337 supplier, Selective, β3-adrenoceptor, b3-adrenoceptor, antagonists, β3-adrenergic, b3-adrenergic, Receptors, Adrenoceptors, L748337, Adrenergic, Beta-3, 2760, Tocris Bioscience
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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.