Nepicastat (hydrochloride)

Modify Date: 2025-08-25 09:13:18

Nepicastat (hydrochloride) Structure
Nepicastat (hydrochloride) structure
Common Name Nepicastat (hydrochloride)
CAS Number 170151-24-3 Molecular Weight 331.812
Density N/A Boiling Point N/A
Molecular Formula C14H16ClF2N3S Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of Nepicastat (hydrochloride)


Nepicastat Hcl(SYN117 Hcl; RS-25560-197 Hcl) is a dopamine beta-hydroxylase inhibitor with IC50 of 8.5 ± 0.8 and 9.0 ± 0.8 nM for bovine and human, respectively. IC50 value: 8.5/9.0 nM(bovine/human dopamine beta-hydroxylase)Dopamine beta-hydroxylase is an enzyme that catalyzes the conversion of dopamine to norepinephrine. Nepicastat (SYN117; RS-25560-197) has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated as such.

 Names

Name 4-(aminomethyl)-3-[(2S)-5,7-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]-1H-imidazole-2-thione,hydrochloride
Synonym More Synonyms

 Nepicastat (hydrochloride) Biological Activity

Description Nepicastat Hcl(SYN117 Hcl; RS-25560-197 Hcl) is a dopamine beta-hydroxylase inhibitor with IC50 of 8.5 ± 0.8 and 9.0 ± 0.8 nM for bovine and human, respectively. IC50 value: 8.5/9.0 nM(bovine/human dopamine beta-hydroxylase)Dopamine beta-hydroxylase is an enzyme that catalyzes the conversion of dopamine to norepinephrine. Nepicastat (SYN117; RS-25560-197) has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated as such.
Related Catalog
References

[1]. 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.

[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]. 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.Circulation. 2000 Oct 17;102(16):1990-5.

[4]. 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.

 Chemical & Physical Properties

Molecular Formula C14H16ClF2N3S
Molecular Weight 331.812
Exact Mass 331.072144
PSA 78.83000
LogP 4.51490
Appearance of Characters white to beige
Storage condition ?20°C
Water Solubility DMSO: soluble10mg/mL, clear

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Hazard Codes Xi
Risk Phrases 36/37/38
Safety Phrases 26
RIDADR NONH for all modes of transport

 Synonyms

Nepicastat HCl
SYN117
Nepitat HCl
Nepicastat hydrochloride
UNII-3WK068D17I
5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione hydrochloride (1:1)
2H-Imidazole-2-thione, 5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-, hydrochloride (1:1)
Nepitat hydrochloride
Nepicastat (hydrochloride)
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Price: $92/10mM*1mLinDMSO

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