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Nepicastat hydrochloride

Cat. No. M1910
Nepicastat hydrochloride Structure


Size Price Availability Quantity
5mg USD 54  USD60 In stock
10mg USD 88.2  USD98 In stock
50mg USD 261  USD290 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Nepicastat hydrochloride (SYN117, RS-25560-197) is an inhibitor of dopamine beta-hydroxylase that catalyzes the conversion of dopamine to norepinephrine. Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity in vitro. In vivo, Nepicastat hydrochloride increases dopamine content and dopamine/noradrenaline ratio in a dose-dependent manner. Nepicastat hydrochloride also produces the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. Nepicastat is currently in Phase II clinical trials in patients with Posttraumatic Stress Disorder.

Cell Experiment
Cell lines
Preparation method
Incubation time
Animal Experiment
Animal models spontaneously hypertensive rats (SHRs)
Formulation water
Dosages 3, 10, 30 or 100 mg/kg
Administration p.o.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 331.81
Formula C14H15F2N3S.HCl
CAS Number 170151-24-3
Purity >99%
Solubility DMSO 56 mg/mL
Storage at -20°C

Disulfiram attenuates drug-primed reinstatement of cocaine seeking via inhibition of dopamine β-hydroxylase.
Schroeder JP, et al. Neuropsychopharmacology. 2010 Nov;35(12):2440-9. PMID: 20736996.

Effects of dopamine beta-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure.
Sabbah HN, et al. Circulation. 2000 Oct 17;102(16):1990-5. PMID: 11034950.

Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase.
Stanley WC, et al. Br J Pharmacol. 1997 Aug;121(8):1803-9. PMID: 9283721.

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Keywords: Nepicastat hydrochloride, SYN117 supplier, Dopamine Receptor, inhibitors

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