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Submit ReviewA 61603 hydrobromide is a potent α-adrenoceptor agonist that is at least 35-fold more potent at α1A than at α1B or α1D sites. Induces dose response increases in spontaneous Ca2+ transients in rat ventricular myocytes in vitro (EC50 = 6.9 nmol/L).
分子量 | 390.29 |
公式 | C14H19N3O3S.HBr |
储存 | Desiccate at +4°C |
CAS Number | 107756-30-9 |
PubChem ID | 9865178 |
InChI Key | LRFLWCZMTGTUEP-UHFFFAOYSA-N |
Smiles | Br.CS(=O)(=O)NC1=C(O)C=CC2=C1CCCC2C1=NCCN1 |
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 | 50 |
以下数据基于产品分子量 390.29。 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 |
---|---|---|---|
0.5 mM | 5.12 mL | 25.62 mL | 51.24 mL |
2.5 mM | 1.02 mL | 5.12 mL | 10.25 mL |
5 mM | 0.51 mL | 2.56 mL | 5.12 mL |
25 mM | 0.1 mL | 0.51 mL | 1.02 mL |
参考文献是支持产品生物活性的出版物。
Knepper et al (1995) A-61603, a potent α1-adrenergic receptor agonist, selective for the α1A receptor subtype. J.Pharmacol.Exp.Ther. 274 97 PMID: 7616455
Luo et al (2007) Receptor subtype involved in α1A-adrenergic receptor-mediated Ca2+ signaling in cardiomyocytes. Acta.Pharmacol.Sin. 28 968 PMID: 17588332
Meyer et al (1996) Synthesis and in vitro characterisation of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective α1A receptor agonist. J.Med.Chem. 39 4116 PMID: 8831777
If you know of a relevant reference for A 61603 hydrobromide, please let us know.
关键词: A 61603 hydrobromide, A 61603 hydrobromide supplier, α1A-adrenoceptor, alpha1A-adrenoceptor, agonists, α1a-adrenergic, alpha1a-adrenergic, a1a-adrenergic, a1a-adrenoceptor, Receptors, A61603, hydrobromide, α1a, Adrenergic, Alpha-1, 1052, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 A 61603 hydrobromide 的部分引用包括:
Thomas et al (2016) A Myocardial Slice Culture Model Reveals Alpha-1A-Adrenergic Receptor Signaling in the Human Heart. JACC Basic Transl Sci 1 155 PMID: 27453955
Jensen et al (2010) Functional alpha-1B adrenergic receptors on human epicardial coronary artery endothelial cells. Naunyn Schmiedebergs Arch Pharmacol 382 475 PMID: 20857090
Thomas et al (2016) The α-1A Adrenergic Receptor in the Rabbit Heart. Nephrol Dial Transplant 11 e0155238 PMID: 27258143
Desir and Peixoto (2014) Renalase in hypertension and kidney disease. Circ Res 29 42604 PMID: 24137013
Treen et al (2016) Divergent regulation of ER and kiss genes by 17 beta -OE in hypothalamic ARC versus AVPV models. Mol.Endocrinol. 30 217 PMID: 26726951
Dash et al (2011) A molecular MRI probe to detect treatment of cardiac apoptosis in vivo. Magn Reson Med 66 1152 PMID: 21360750
O-Uchi et al (2008) Interaction of α1-adrenoceptor subtypes with different G proteins induces opposite effects on cardiac L-type Ca2+ channel. PLoS One 102 1378 PMID: 18467629
Jensen et al (2009) The α-1D Is the predominant α-1-adrenergic receptor subtype in human epicardial coronary arteries. PLoS One 54 1137 PMID: 19761933
Montgomery (2017) An Alpha-1A Adrenergic Receptor Agonist Prevents Acute dox. Cardiomyopathy in Male Mice. Plos One 12 e0168409 PMID: 28081170
Copik et al (2015) Isoproterenol acts as a biased agonist of the α-1A-adrenoceptor that selectively activates the MAPK/ERK pathway. PLoS One 10 e0115701 PMID: 25606852
Amirak et al (2013) p90 ribosomal S6 kinases play a significant role in early gene regulation in the cardiomyocyte response to G(q)-protein-coupled receptor stimuli, endothelin-1 and α(1)-adrenergic receptor agonists. Biochem J 450 351 PMID: 23215897
Rokosh and Simpson (2002) Knockout of the alpha 1A/C-adrenergic receptor subtype: the alpha 1A/C is expressed in resistance arteries and is required to maintain arterial blood pressure. Proc Natl Acad Sci U S A 99 9474 PMID: 12093905
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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.