Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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.
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 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 33.2 mg/mL (100 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
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