Nepicastat hydrochloride

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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