1. Metabolic Enzyme/Protease
  2. Dopamine β-hydroxylase
  3. Nepicastat hydrochloride

Nepicastat hydrochloride (Synonyms: SYN-117 hydrochloride; RS-25560-197 hydrochloride)

Cat. No.: HY-13289A Purity: 99.98%
Handling Instructions

Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB).

For research use only. We do not sell to patients.

Nepicastat hydrochloride Chemical Structure

Nepicastat hydrochloride Chemical Structure

CAS No. : 170151-24-3

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10 mM * 1 mL in DMSO USD 66 In-stock
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100 mg USD 800 In-stock
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Description

Nepicastat hydrochloride (SYN-117 hydrochloride) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat hydrochloride produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat hydrochloride can cross the blood-brain barrier (BBB)[1][2][3].

IC50 & Target

IC50: 8.5 nM (bovine dopamine-beta-hydroxylase), 9 nM (human dopamine-beta-hydroxylase)[2]

In Vivo

Nepicastat hydrochloride (SYN-117 hydrochloride) (3-100 mg/kg; p.o.; three consecutive times, 12 hours apart times) produces dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle[3].

Animal Model: 15-16 weeks male spontaneously hypertensive rats (SHRs)[3]
Dosage: 3, 10, 30, 100 mg/kg
Administration: Oral administration; three consecutive times, 12 hours apart
Result: Produced dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery (mesenteric or renal), left ventricle and cerebral cortex.
Clinical Trial
Molecular Weight

331.81

Formula

C₁₄H₁₆ClF₂N₃S

CAS No.

170151-24-3

SMILES

FC1=CC(F)=C2CC[[email protected]@H](CC2=C1)N3C(CN)=CNC3=S.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6 mg/mL (18.08 mM; Need ultrasonic)

H2O : 2 mg/mL (6.03 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0138 mL 15.0689 mL 30.1377 mL
5 mM 0.6028 mL 3.0138 mL 6.0275 mL
10 mM 0.3014 mL 1.5069 mL 3.0138 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.6 mg/mL (1.81 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.6 mg/mL (1.81 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.6 mg/mL (1.81 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.98%

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Keywords:

NepicastatSYN-117RS-25560-197SYN117SYN 117Dopamine β-hydroxylaseDopamine beta-hydroxylaseDopamine beta-monooxygenaseDopamine β-monooxygenaseInhibitorinhibitorinhibit

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Product name:
Nepicastat hydrochloride
Cat. No.:
HY-13289A
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