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Nepicastat hydrochloride

Catalog No. T6604   CAS 170151-24-3
Synonyms: SYN-117 hydrochloride, RS-25560-197 hydrochloride, 内匹司他盐酸盐, Nepicastat HCl, Nepicastat (SYN-117) HCl

Nepicastat (SYN-117) HCl 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.

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Nepicastat hydrochloride, CAS 170151-24-3
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Nepicastat (SYN-117) HCl 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 HμMan dopamine-beta-hydroxylase:9 nM, Bovine dopamine-beta-hydroxylase: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 SYN-117 hydrochloride, RS-25560-197 hydrochloride, 内匹司他盐酸盐, Nepicastat HCl, Nepicastat (SYN-117) HCl
Molecular Weight 331.81
Formula C14H16ClF2N3S
CAS No. 170151-24-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 33.2 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

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:
Anti-Cancer Compound Library Anti-Parkinson's Disease Compound Library Inhibitor Library Anti-Metabolism Disease Compound Library Fluorochemical Library Drug Repurposing Compound Library Neuronal Signaling Compound Library CNS-Penetrant Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library

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Related compounds with same targets
(R)-Nepicastat HCl Telotristat Etiprate Osilodrostat pCPA methyl ester hydrochloride Mildronate LX-1031 LPA2 antagonist 1 GSK180

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Keywords

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