Nepicastat hydrochloride

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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)
Citations (1)

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
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 Data for Nepicastat hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.01 mL 15.07 mL 30.14 mL
5 mM 0.6 mL 3.01 mL 6.03 mL
10 mM 0.3 mL 1.51 mL 3.01 mL
50 mM 0.06 mL 0.3 mL 0.6 mL

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Product Datasheets for Nepicastat hydrochloride

References for Nepicastat hydrochloride

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

Manvich et al (2013) DA 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 DA 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 DA-beta-hydroxylase. Br.J.Pharmacol. 121 1803 PMID: 9283721

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Keywords: Nepicastat hydrochloride, Nepicastat hydrochloride supplier, dopamine, beta-hydroxylase, inhibitors, inhibits, β, B-hydroxylase, DBH, noradrenaline, norepinephrine, potent, selective, orally, bioavailable, Hydroxylases, 5037, Tocris Bioscience

1 Citation for Nepicastat hydrochloride

Citations are publications that use Tocris products. Selected citations for Nepicastat hydrochloride include:

Armando et al (2021) Synergistic Growth Inhibition of HT-29 Colon and MCF-7 Breast Cancer Cells with Simultaneous and Sequential Combinations of Antineoplastics and CNS Drugs. Int J Mol Sci 22 PMID: 34299028

Do you know of a great paper that uses Nepicastat hydrochloride from Tocris? Please let us know.

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