Nepicastat hydrochloride

Name: Nepicastat hydrochloride
Brand: Tocris Bioscience
SKU: 5037

Tocris Bioscience, part of Bio-Techne | Catalog # 5037

Citations (1)

COA / SDS

Potent and selective dopamine β-hydroxylase (DBH) inhibitor; orally bioavailable

Key Product Details

Description:	Potent and selective dopamine β-hydroxylase (DBH) inhibitor; orally bioavailable
Chemical Name:	5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	331.81

View Full Technical Details for Nepicastat hydrochloride

Technical Data
Citations

Biological Activity for Nepicastat hydrochloride

Nepicastat hydrochloride is a 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 for Nepicastat hydrochloride

M. Wt	331.81
Formula	C₁₄H₁₅F₂N₃S.HCl
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	170151-24-3
PubChem ID	9840545
InChi Key	DIPDUAJWNBEVOY-PPHPATTJSA-N
Smiles	S=C(NC=C3CN)N3[C@H]2CCC1=C(F)C=C(F)C=C1C2.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Nepicastat hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	33.18	100

Preparing Stock Solutions for Nepicastat hydrochloride

The following data is based on the product molecular weight 331.81.

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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.01 mL	15.07 mL	30.14 mL
5 mM	0.60 mL	3.01 mL	6.03 mL
10 mM	0.30 mL	1.51 mL	3.01 mL
50 mM	0.06 mL	0.30 mL	0.60 mL

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References for Nepicastat hydrochloride

References are publications that support the biological activity of the product.

Sabbah Effects of DA β-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. Circulation 2000 PMID: 11034950
Stanley Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of DA-beta-hydroxylase. Br.J.Pharmacol. 1997 PMID: 9283721
Manvich DA β-hydroxylase inhibitors enhance the discriminative stimulus effects of cocaine in rats. J.Pharmacol.Exp.Ther. 2013 PMID: 24068832