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Nepicastat (SYN-117) HCl

In stock
Catalog No.
A4332
Dopamine-β-hydroxylase inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$77.00
In stock
5mg
$70.00
In stock
10mg
$120.00
In stock
50mg
$540.00
In stock

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Background

Nepicastat (SYN-117) HCl is a potent and selective inhibitor of dopamine-β-hydroxylase with IC50 values of 8.5 and 9.0 nM in bovine and human, respectively [1].

Dopamine-β-hydroxylase is an enzyme involved in the synthesis of small-molecule membrane-bound neurotransmitters. Dopamine-β-hydroxylase catalyses the synthesis of noradrenaline [1].

Nepicastat (SYN-117) HCl is a potent and selective dopamine-β-hydroxylase inhibitor. (R)-Nepicastat exhibited 2-3 fold less potent than nepicastat [1].

In beagle dogs and spontaneously hypertensive rats, nepicastat reduced noradrenaline in a dose-dependent way and increased dopamine and dopamine/noradrenaline ratio in cerebral cortex, left ventricle and the artery. In beagle dogs, nepicastat (2 mg/kg) significantly reduced noradrenaline by 52% and increased dopamine by 646% and dopamine/noradrenaline ratio in plasma [1]. In pithed spontaneously hypertensive rats, nepicastat inhibited the pressor and positive chronotropic due to preganglionic sympathetic nerve stimulation. In spontaneously hypertensive rats, nepicastat (3 mg/kg) exhibited antihypertensive effects and reduced renal vascular resistance by 38% [2]. In rats, nepicastat significantly increased extracellular dopamine accumulation induced by cocaine and amphetamine in the medial prefrontal cortex [3].

References:
[1].  Stanley WC, Li B, Bonhaus DW, et al. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. Br J Pharmacol, 1997, 121(8): 1803-1809.
[2].  Stanley WC, Lee K, Johnson LG, et al. Cardiovascular effects of nepicastat (RS-25560-197), a novel dopamine beta-hydroxylase inhibitor. J Cardiovasc Pharmacol, 1998, 31(6): 963-970.
[3].  Devoto P, Flore G, Saba P, et al. The dopamine beta-hydroxylase inhibitor nepicastat increases dopamine release and potentiates psychostimulant-induced dopamine release in the prefrontal cortex. Addict Biol, 2014, 19(4): 612-622.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt331.81
Cas No.170151-24-3
FormulaC14H15F2N3S.HCl
Solubility≥16.6 mg/mL in DMSO, <2.58 mg/mL in EtOH, <2.27 mg/mL in H2O
Chemical Name4-(aminomethyl)-3-[(2S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1H-imidazole-2-thione;hydrochloride
SDFDownload SDF
Canonical SMILESC1CC2=C(C=C(C=C2CC1N3C(=CNC3=S)CN)F)F.Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Biological Activity

Description Nepicastat is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 values of 8.5 nM and 9 nM, respectively.
Targets bovine dopamine-β-hydroxylase human dopamine-β-hydroxylase        
IC50 8.5 nM 9 nM        

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