Nepicastat hydrochloride

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Cat.No. 5037 - Nepicastat hydrochloride | C14H15F2N3S.HCl | CAS No. 170151-24-3
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)

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 331.81. Batch specific molecular weights may vary from batch to batch due to solvent 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 0.6 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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References are publications that support the products' biological activity.

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, Hydroxylases, Hydroxylases, Tocris Bioscience

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