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Nepicastat hydrochloride

Chemical Structure : Nepicastat hydrochloride

CAS No.: 170151-24-3

Nepicastat hydrochloride (SYN117 hydrochloride, RS-25560-197 hydrochloride)

货号: PC-43467Not For Human Use, Lab Use Only.

Nepicastat (RS-25560-197, SYN117) hydrochloride is a potent, selective, orally active inhibitor of dopamine-beta-hydroxylase (DBH) with IC50 of 8.5 and 9.0 nM for bovine and human DBH, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Nepicastat (RS-25560-197, SYN117) hydrochloride is a potent, selective, orally active inhibitor of dopamine-beta-hydroxylase (DBH) with IC50 of 8.5 and 9.0 nM for bovine and human DBH, respectively.
Nepicastat is 2-3 fold more potent than the corresponding R-enantiomer (RS-25560-198).
Nepicastat produces dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery, left ventricle and cerebral cortex in spontaneously hypertensive rats.

物理化学性质&存储条件

分子量 331.81
分子式 C14H16ClF2N3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 31 mg/mL

Chemical Name/SMILES

2H-Imidazole-2-thione, 5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-, hydrochloride (1:1)

参考文献

1. Stanley WC, et al. Br J Pharmacol. 1997 Aug;121(8):1803-9.

2. Stanley WC, et al. J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70.

3. Sabbah HN, et al. Circulation. 2000 Oct 17;102(16):1990-5.

4. Schroeder JP, et al. Neuropsychopharmacology. 2010 Nov;35(12):2440-9.

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