(R) -Nepicastat (hydrochloride)

(R) -Nepicastat hydrochloride is the isomer of Nepicastat (HY-13289) . Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB) [1][2][3].

Product Specifications

CAS Number

[195881-94-8]

Product Name Alternative

(R) -SYN117 (hydrochloride) ; (R) -RS-25560-197 (hydrochloride) ; RS-25560-198 (hydrochloride)

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Dopamine β-hydroxylase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/r-nepicastat-hydrochloride.html

Smiles

S=C1NC=C(CN)N1[C@H]2CC3=C(C(F)=CC(F)=C3)CC2.Cl

Molecular Formula

C14H16ClF2N3S

Molecular Weight

331.81

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

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. 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.|[3]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.|[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.