Nepicastat hydrochloride

Cat. No. 5037

Nepicastat hydrochloride C14H15F2N3S.HCl [170151-24-3]

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Chemical Name: 5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione hydrochloride

Biological Activity

Potent and selective dopamine β-hydroxylase (DBH) inhibitor (IC50 = 9 nM) . Selective for DBH over 12 other enzymes. Decreases noradrenaline and increases dopamine levels in tissues and plasma in hypertensive rats. Prevents progressive left ventricular dysfunction in an in vivo heart failure model. Also potentiates the stimulus effects of cocaine without producing cocaine-like effects in rats. Orally bioavailable.

Technical Data

M.Wt:
331.81
Formula:
C14H15F2N3S.HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
170151-24-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Manvich et al (2013) Dopamine β-hydroxylase inhibitors enhance the discriminative stimulus effects of cocaine in rats. J.Pharmacol.Exp.Ther. 347 564. PMID: 24068832.

Sabbah et al (2000) Effects of dopamine β-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. Circulation 102 1990. PMID: 11034950.

Stanley et al (1997) Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. Br.J.Pharmacol. 121 1803. PMID: 9283721.

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Keywords: Nepicastat hydrochloride, supplier, dopamine, beta-hydroxylase, inhibitors, inhibits, β, B-hydroxylase, DBH, noradrenaline, norepinephrine, potent, selective, orally, bioavailable, DBH, Tocris Bioscience, Hydroxylase Inhibitor products

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