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A 61603 hydrobromide

Catalog No.GC14527

A 61603 hydrobromide Chemical Structure

α-adrenoceptor agonist

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1mg
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10mg
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Sample solution is provided at 25 µL, 10mM.

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Background

A 61603 hydrobromide is a potent and selective agonist of α1A-adrenoceptor [1].

α1A-adrenoceptor (α1A-AR) belongs to α1- adrenergic receptors, which include three subtypes α1A, α1B and α1D and play an important role in regulating cell growth and proliferation.

A 61603 hydrobromide is a potent and selective α1A-adrenoceptor agonist. A-61603 was 35-fold more potent at α1A-AR than at α1B-AR or α1D-AR. In fibroblast cells transfected with α1A-AR, A-61603 significantly stimulated phosphoinositide hydrolysis [1]. A 61603 exhibited affinity for α1A-AR, α1B-AR and α1D-AR with pKi values of 8.05/7.52, 5.68 and 5.87, respectively. Also, A 61603 exhibited agonist activities for α1A-AR, α1B-AR and α1D-AR with pEC50 values of 8.24/7.66, 6.50 and 5.59, respectively [2]. In neonatal rat ventricular myocytes, A61603 significantly increased the frequency of Ca2+ transients with EC50 value of 6.9 nM in a dose-dependent way [3]. In mesenteric vascular bed isolated from mice, A61603 significantly increased perfusion pressure with 235-fold higher potency than phenylephrine, which suggested that α1A-AR plays an important role in the control of blood pressure [4].

References:
[1].  Knepper SM, Buckner SA, Brune ME, et al. A-61603, a potent alpha 1-adrenergic receptor agonist, selective for the alpha 1A receptor subtype. J Pharmacol Exp Ther, 1995, 274(1): 97-103.
[2].  Meyer MD, Altenbach RJ, Hancock AA, et al. Synthesis and in vitro characterization 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 alpha 1A receptor agonist. J Med Chem, 1996, 39(20): 4116-4119.
[3].  Luo DL, Gao J, Fan LL, et al. Receptor subtype involved in alpha 1-adrenergic receptor-mediated Ca2+ signaling in cardiomyocytes. Acta Pharmacol Sin, 2007, 28(7): 968-974.
[4].  Martínez-Salas SG1, Campos-Peralta JM, Pares-Hipolito J, et al. Alpha1A-adrenoceptors predominate in the control of blood pressure in mouse mesenteric vascular bed. Auton Autacoid Pharmacol, 2007, 27(3): 137-142.

Chemical Properties

Cas No. 107756-30-9 SDF
Chemical Name (S)-N-(5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)methanesulfonamide hydrobromide
Canonical SMILES OC1=C(C2=C(C=C1)[C@@H](C3=NCCN3)CCC2)NS(=O)(C)=O.Br
Formula C14H19N3O3S.HBr M.Wt 390.29
Solubility DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 10 mg/ml Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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