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Nepicastat

Nepicastat

Item no.	HY-13289-10mg
Manufacturer	MedChem Express
CASRN	173997-05-2
Amount	10 mg
Quantity options	100 mg 10 mg 1 ea 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Citations	bioRxiv. 2021 Mar 4. Commun Biol. 2022 Jan 25;5(1):96. Cell Rep Med. 2024 Oct 1:101771. [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.
Smiles	FC1=CC(F)=C2CC[C@@H](CC2=C1)N3C(CN)=CNC3=S
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	SYN117,RS-25560-197
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Neuroscience-Neuromodulation
Manufacturer - Targets	Dopamine β-hydroxylase
Shipping Temperature	Room temperature
Molecular Weight	295.3508064
Product 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].
Manufacturer - Research Area	Cardiovascular Disease
Solubility	DMSO : ≥ 48 mg/mL
Manufacturer - Pathway	Metabolic Enzyme/Protease
Clinical information	Phase 2

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