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    (R)-Nepicastat HCl [RS-25560-198 HCl]
    (R)-Nepicastat HCl [RS-25560-198 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 #: V0937
    CAS #: 195881-94-8Purity ≥98%

    Description: (R)-Nepicastat HCl (also known as RS-25560-198 HCl), the R-enantiomer of Nepicastat HCl, is a potent and selective inhibitor with IC50 of 25.1 nM and 18.3 nM for bovine and human dopamine-β-hydroxylase, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. 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.

    Related CAS:  170151-24-3 (Nepicastat HCl)

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    Molecular Weight (MW)331.81
    FormulaC14H15F2N3S.HCl
    CAS No.195881-94-8
    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
    Solubility (In vivo)30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL  
    SynonymsRS-25560-198 HCl; RS-25560 198 HCl; RS 25560-198 HCl; RS25560-198 HCl
    SMILES CodeS=C1N([[email protected]]2CC3=C(C(F)=CC(F)=C3)CC2)C(CN)=CN1.[H]Cl


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    In Vitro

    In vitro activity: (R)-Nepicastat produces concentration-dependent inhibition of bovine and human dopamine-β-hydroxylase activity in vitro.

    In Vivo(R)-Nepicastat (30 mg/kg, p.o.) reduces noradrenaline content, dopamine content and dopamine/noradrenaline ratio in mesenteric artery and left ventricle of spontaneously hypertensive rats (SHRs).
    Animal modelAnimal Models Spontaneously hypertensive rats (SHRs).
    Formulation & DosageDissolved in distilled water; 30 mg/kg; p.o.
    References

    Br J Pharmacol. 1997 Aug;121(8):1803-9.


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

    (R)-Nepicastat HClFigure 2Effects 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.
    (R)-Nepicastat 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


     

     

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


    (R)-Nepicastat 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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