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(R) -Nepicastat (hydrochloride)

(R) -Nepicastat hydrochloride is the isomer of Nepicastat. 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)[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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