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    Nepicastat (SYN-117) HCl
    Nepicastat (SYN-117) HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0932
    CAS #: 170151-24-3Purity ≥98%

    Description: Nepicastat HCl (also known as SYN117 and RS-25560-197) is a potent and selective inhibitor of both bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Dopamine beta-hydroxylase is an enzyme that catalyzes the conversion of dopamine to norepinephrine.Nepicastat has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated.

    References: Br J Pharmacol. 1997 Aug;121(8):1803-9; J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70.

    Related CAS #: 170151-24-3 (HCl); 173997-05-2 (free base);  195881-94-8 (HCl R isomer) 

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    Molecular Weight (MW)331.81
    FormulaC14H15F2N3S.HCl
    CAS No.170151-24-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 66 mg/mL (198.9 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILES CodeS=C1NC=C(CN)N1[[email protected]@H]2CC3=C(C(F)=CC(F)=C3)CC2.[H]Cl
    SynonymsSYN117; SYN-117; SYN 117; RS25560197; RS25560-197; RS-25560-197; RS 25560-197; Nepicastat; Nepicastat HCl


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    In Vitro

    In vitro activity: In vitro, Nepicastat hydrochloride shows the selective and concentration-dependent inhibition effects on bovine and human dopamine-beta-hydroxylase activity with IC50 of 8.5 nM and 9.0 nM, respectively. While Nepicastat hydrochloride has negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors.

    In VivoIn the artery, left ventricle and cerebral cortex of spontaneously hypertensive rats (SHRs), Nepicastat hydrochloride reduces noradrenaline content, and increases dopamine content and dopamine/noradrenaline ratio in a dose-dependent manner. In addition, Nepicastat hydrochloride also produces the similar effects on noradrenaline, dopamine and dopamine/noradrenaline ratio in tissues and plasma of beagle dogs. In inactin-anesthetized SHRs, Nepicastat hydrochloride (3 mg/kg, i.v.) produces the antihypertensive effects and causes a significant decrease in renal vascular resistance (38%) and an increase in renal blood flow (22%). In dogs with chronic heart failure, low-dose Nepicastat hydrochloride (0.5 mg/kg) prevents left ventricular (LV) dysfunction and remodeling, and combination therapy of Nepicastat hydrochloride and enalapril results in additional improvements in all morphological features. In rat brain, Nepicastat hydrochloride at a dose of 50 mg/kg ( i.p.) leads to the reduction of norepinephrine (NE) and blocks cocaine-primed reinstatement of cocaine seeking.
    Animal modelSpontaneously hypertensive rats (SHRs).
    Formulation & DosageDissolved in distilled water; 100 mg/kg; p.o.
    References

    Br J Pharmacol. 1997 Aug;121(8):1803-9; J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Nepicastat (SYN-117) HClEffects of nepicastat on tissue noradrenaline (NA) and dopamine (DA) content in the mesenteric artery (a), left ventricle (b) and cerebral cortex (c) of SHRs. Br J Pharmacol.1997 Aug;121(8):1803-9. 
    Nepicastat (SYN-117) HCl
    Effects of nepicastat on tissue noradrenaline (NA) and dopamine (DA) content in renal artery (a), left ventricle (b) and cerebral cortex (c) of beagle dogs.  Br J Pharmacol.1997 Aug;121


     

     

     Nepicastat (SYN-117) HClEffects of nepicastat on tissue dopamine/noradrenaline ratio in the mesenteric artery, left ventricle and cerebral cortex of SHRs.



    Nepicastat (SYN-117) HCl
    Effects of nepicastat on tissue noradrenaline (NA) and dopamine (DA) content in renal artery (a), left ventricle (b) and cerebral cortex (c) of beagle dogs.  Br J Pharmacol.1997 Aug;121


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