Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 12,000 | |||
10 mg | 在庫あり | ¥ 20,500 | |||
25 mg | 在庫あり | ¥ 36,500 | |||
50 mg | 在庫あり | ¥ 62,500 | |||
100 mg | 在庫あり | ¥ 109,500 | |||
500 mg | 在庫あり | ¥ 241,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 13,000 |
説明 | 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. |
ターゲット&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] |
別名 | Nepicastat HCl, RS-25560-197 hydrochloride, SYN-117 hydrochloride, Nepicastat (SYN-117) HCl |
分子量 | 331.81 |
分子式 | C14H15F2N3S·HCl |
CAS No. | 170151-24-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 33.2 mg/mL (100 mM)
You can also refer to dose conversion for different animals. 詳細
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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 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