Nepicastat

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Nepicastat (RS-25560-197, SYN-117) 是一种有效的、选择性的、口服活性的多巴胺-β-羟化酶 (DBH) 抑制剂，对牛和人 DBH 的 IC50 分别为 8.5 和 9.0 nM。

Nepicastat (RS-25560-197, SYN-117) 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); 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.Hypertension Discontinued.

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Nepicastat (3-100 mg/kg; p.o.; three consecutive times, 12 hours apart times) produces dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle. Animal Model:15-16 weeks male spontaneously hypertensive rats (SHRs)Dosage:Oral administration; three consecutive times, 12 hours apart Administration:3, 10, 30, 100 mg/kg Result:Produced dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle and cerebral cortex.

SYN117 | RS-25560-197 | SYN-117 | SYN 117

Metabolic Enzyme/Protease

Dopamine beta-hydroxylase

Dopamine beta-hydroxylase

Cardiovascular Disease

Hypertension

173997-05-2

295.35

C14H15F2N3S

>98% (HPLC)

DMSO: ≥ 48 mg/mL

C1CC2=C(CC1N3C(=CNC3=S)CN)C=C(C=C2F)F

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

(-20℃)

With Ice Pack

≥ 2 years