Nepicastat hydrochloride

SKU: orb1300622

Description

Nepicastat hydrochloride

Research Area

Metabolism Research

Key Properties

• CAS Number: 170151-24-3
• MW: 331.81
• Purity: 99.81%
• Formula: C₁₄H₁₅F₂N₃S·HCl
• SMILES: Cl.NCc1c[nH]c(=S)n1[C@H]1CCc2c(F)cc(F)cc2C1
• Target: Hydroxylase
• Solubility: DMSO:50 mg/mL (150.69 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (3.01 mM)

Bioactivity

• Target IC50:
  DBH (bovine):8.5 nM|DBH (human):9 nM
• In Vivo:
  I 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 produce the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. In inactin-anesthetized SHRs, Nepicastat hydrochloride (3 mg/kg, i.v.) produce the antihypertensive effects and causes a significant decrease in renal vascular resistance (38%) and an increase in renal blood flow (22%). 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. 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.
• In Vitro:
  In vitro, Nepicastat hydrochloride show 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Dopamine β-hydroxylase, Dopamine β-monooxygenase, Dopamine beta-hydroxylase, Dopamine beta-monooxygenase, Inhibitor, Nepicastat, Nepicastat (SYN-117) HCl, Nepicastat HCl, Nepicastat hydrochloride, Nepicastat Hydrochloride, inhibit, SYN 117, SYN 117 Hydrochloride, SYN117, SYN-117, SYN117 Hydrochloride, SYN-117 hydrochloride, SYN-117 Hydrochloride, RS-25560-197 Hydrochloride, RS-25560-197 hydrochloride

Compound Identifiers

PubChem CID

9840545