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Nepicastat

CAT: 0804-HY-13289Size: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-13289Size:1 Each
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Description
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].
CAS Number
173997-05-2
Product Name Alternative
SYN117; RS-25560-197
UNSPSC
12352005
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/nepicastat.html
Solubility
DMSO : ≥ 48 mg/mL
Smiles
FC1=CC(F)=C2CC[C@@H](CC2=C1)N3C(CN)=CNC3=S
Molecular Formula
C14H15F2N3S
Molecular Weight
295.35
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
Phase 2
Citation 01
BioRxiv. 2021 Mar 4.|Commun Biol. 2022 Jan 25;5 (1) :96.|Cell Rep Med. 2024 Oct 1:101771.

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