Free shipping on all orders over $ 500

Nepicastat hydrochloride

Cat. No. M1910
Nepicastat hydrochloride Structure
Synonym:

SYN117

Size Price Availability Quantity
5mg USD 54  USD60 In stock
10mg USD 88.2  USD98 In stock
50mg USD 261  USD290 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
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
References

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.

Related Dopamine Receptor Products
ML417

ML417 is a highly selective and brain penetrant D3 dopamine receptor (D3R) agonist, with EC50 of 38 nM.

Cariprazine

Cariprazine is a D2 and D3 receptor partial agonist, with high selectivity towards the D3 receptor.

PD-168077 maleate

PD-168077 maleate is a potent D4 dopamine receptor agonist (Ki = 8.7 nM), with > 400-fold and > 300-fold selectivity over D2 / D3 subtypes, respectively.

SCH23390

SCH23390 is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively).

MPTP HCl

MPTP hcl is a compound to the neurotoxin MPP+ which causes permanent symptoms of Parkinson's disease.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.