Free shipping on all orders over $ 500

Nepicastat hydrochloride

Cat. No. M1910
Nepicastat hydrochloride Structure


Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 98  USD98 In stock
50mg USD 290  USD290 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
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.

Protocol (for reference only)
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.
Chemical Information
Molecular Weight 331.81
Formula C14H15F2N3S.HCl
CAS Number 170151-24-3
Solubility (25°C) DMSO 56 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.


[1] Schroeder JP, et al. Neuropsychopharmacology. Disulfiram attenuates drug-primed reinstatement of cocaine seeking via inhibition of dopamine β-hydroxylase.

[2] Sabbah HN, et al. Circulation. Effects of dopamine beta-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure.

[3] Stanley WC, et al. Br J Pharmacol. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase.

Related Dopamine Receptor Products

Cyclo(glycyl-L-leucyl) (Cyclo(leu-gly)), a neuropeptide, down-regulates dopamine (DA) receptors and attenuates dopaminergic supersensitivity.


Onzigolide (BIM-23A760), a chimeric dopamine-somatostatin compound, shows potent agonist activity at both DA type 2 (D2R) and SST type 2 (SSTR2) receptors.


CVL-871 is a partial agonist at dopamine D1/5 receptors and may be used in dementia-related studies.

Paliperidone palmitate

Paliperidone palmitate is the ester precursor compound of Paliperidone, a potent dopamine antagonist and 5-HT2A antagonist. Paliperidone is a potent dopamine antagonist and 5-HT2A antagonist.


Melevodopaa is an oral precursor compound to Levodopa that enters the body and can pass through the gut and blood-brain barrier into the brain. In the brain, Melevodopa is converted to dopamine, which increases dopamine levels in the brain and can be used in studies related to Parkinson's disease.

Abmole Inhibitor Catalog

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

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.