Nepicastat hydrochloride

SKU: orb1225959

Description

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(In Vivo):Nepicastat hydrochloride (SYN-117 hydrochloride) (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.

Key Properties

• CAS Number: 170151-24-3
• MW: 331.8
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₆ClF₂N₃S
• SMILES: C1CC2=C(CC1N3C(=CNC3=S)CN)C=C(C=C2F)F.Cl
• Target: Dopamine beta-hydroxylase
• Solubility: DMSO: ≥ 31 mg/mL

Bioactivity

• In Vivo:
  Nepicastat hydrochloride (SYN-117 hydrochloride) (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: 3, 10, 30, 100 mg/kg. Administration: Oral administration; three consecutive times, 12 hours apart. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SYN-117 hydrochloride | RS-25560-197 hydrochloride

Quick Database Links

Gene Symbol

Dopamine beta-hydroxylase