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Nepicastat hydrochloride

Catalog No. T6604 CAS 170151-24-3

Synonyms: Nepicastat HCl, RS-25560-197 hydrochloride, SYN-117 hydrochloride, Nepicastat (SYN-117) HCl

Nepicastat hydrochloride (RS-25560-197 hydrochloride) is an effective and specific inhibitor, which is used for bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, respectively.The affinity of Nepicastat for twelve other enzymes and thirteen neurotransmitter receptors is negligible.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Nepicastat hydrochloride Chemical Structure

Nepicastat hydrochloride, CAS 170151-24-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 52.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 159.00
50 mg	In stock	$ 271.00
100 mg	In stock	$ 476.00
500 mg	In stock	$ 1,050.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 99.81%

Purity: 98.74%

Purity: 98.35%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Nepicastat hydrochloride (RS-25560-197 hydrochloride) is an effective and specific inhibitor, which is used for bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, respectively.The affinity of Nepicastat for twelve other enzymes and thirteen neurotransmitter receptors is negligible.
Targets&IC50	DBH (human):9 nM, DBH (bovine):8.5 nM
In vitro	In vitro, Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity with IC50 of 8.5 nM and 9.0 nM, respectively. While Nepicastat hydrochloride has negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. [1]
In vivo	In the artery, left ventricle and cerebral cortex of spontaneously hypertensive rats (SHRs), Nepicastat hydrochloride reduces noradrenaline content, and increases dopamine content and dopamine/noradrenaline ratio in a dose-dependent manner. In addition, Nepicastat hydrochloride also produces the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. [1] In inactin-anesthetized SHRs, Nepicastat hydrochloride (3 mg/kg, i.v.) produces the antihypertensive effects and causes a significant decrease in renal vascular resistance (38%) and an increase in renal blood flow (22%). [2] In dogs with chronic heart failure, low-dose Nepicastat hydrochloride (0.5 mg/kg) prevents left ventricular (LV) dysfunction and remodeling, and combination therapy of Nepicastat hydrochloride and enalapril results in additional improvements in all morphological features. [3] In rat brain, Nepicastat hydrochloride at a dose of 50 mg/kg ( i.p.) leads to the reduction of norepinephrine (NE) and blocks cocaine-primed reinstatement of cocaine seeking. [4]

Synonyms	Nepicastat HCl, RS-25560-197 hydrochloride, SYN-117 hydrochloride, Nepicastat (SYN-117) HCl
Molecular Weight	331.81
Formula	C14H15F2N3S·HCl
CAS No.	170151-24-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33.2 mg/mL (100 mM)

References and Literature

1. Stanley WC, et al. Br J Pharmacol. 1997, 121(8), 1803-1809. 2. Stanley WC, et al. J Cardiovasc Pharmacol. 1998, 31(6), 963-970. 3. Sabbah HN, et al. Circulation. 2000, 102(16), 1990-1995. 4. Schroeder JP, et al. Neuropsychopharmacology. 2010, 35(12), 2440-2449.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library CNS-Penetrant Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Orally Active Compound Library ReFRAME Related Library Clinical Compound Library

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Keywords

Nepicastat hydrochloride 170151-24-3 Metabolism Hydroxylase Dopamine beta-monooxygenase Dopamine beta-hydroxylase Dopamine β-monooxygenase Nepicastat SYN117 Nepicastat Hydrochloride SYN-117 Dopamine β-hydroxylase Inhibitor RS-25560-197 Hydrochloride SYN 117 Hydrochloride SYN 117 Nepicastat HCl inhibit RS-25560-197 hydrochloride SYN-117 hydrochloride SYN117 Hydrochloride Nepicastat (SYN-117) HCl SYN-117 Hydrochloride inhibitor

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