Nepicastat (hydrochloride)

Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB) [1][2][3].

Product Specifications

CAS Number

[170151-24-3]

Product Name Alternative

SYN-117 hydrochloride; RS-25560-197 hydrochloride

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Dopamine β-hydroxylase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Nepicastat-hydrochloride.html

Concentration

10mM

Purity

99.48

Solubility

DMSO : 6 mg/mL (ultrasonic) |H2O : 2 mg/mL (ultrasonic; warming)

Smiles

FC1=CC(F)=C2CC[C@@H](CC2=C1)N3C(CN)=CNC3=S.Cl

Molecular Formula

C14H16ClF2N3S

Molecular Weight

331.81

Precautions

H302, H315, H319, H335

References & Citations

[1]Beliaev A, et al. Synthesis and biological evaluation of novel, peripherally selective chromanyl imidazolethione-based inhibitors of dopamine beta-hydroxylase.J Med Chem. 2006 Feb 9;49 (3) :1191-7.|[2]Stanley WC, et al. Cardiovascular effects of nepicastat (RS-25560-197), a novel dopamine beta-hydroxylase inhibitor. J Cardiovasc Pharmacol. 1998 Jun;31 (6) :963-70.|[3]Stanley WC, et al. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase. Br J Pharmacol. 1997 Aug;121 (8) :1803-9.|[4]Sabbah HN, et al. Effects of dopamine beta-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure.