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

Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) can cross the blood-brain barrier (BBB).

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

Nepicastat Chemical Structure

Nepicastat Chemical Structure

CAS No. : 173997-05-2

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Description

Nepicastat (SYN117) is a selective, potent, and orally active inhibitor of dopamine-beta-hydroxylase. Nepicastat (SYN117) produces concentration-dependent inhibition of bovine (IC50=8.5 nM) and human (IC50=9 nM) dopamine-beta-hydroxylase. Nepicastat (SYN117) 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 (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 15-16 weeks male spontaneously hypertensive rats (SHRs)[3]
Dosage: Oral administration; three consecutive times, 12 hours apart
Administration: 3, 10, 30, 100 mg/kg
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

295.35

Formula

C14H15F2N3S

CAS No.
SMILES

FC1=CC(F)=C2CC[C@@H](CC2=C1)N3C(CN)=CNC3=S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : ≥ 48 mg/mL (162.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3858 mL 16.9290 mL 33.8580 mL
5 mM 0.6772 mL 3.3858 mL 6.7716 mL
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Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3858 mL 16.9290 mL 33.8580 mL 84.6451 mL
5 mM 0.6772 mL 3.3858 mL 6.7716 mL 16.9290 mL
10 mM 0.3386 mL 1.6929 mL 3.3858 mL 8.4645 mL
15 mM 0.2257 mL 1.1286 mL 2.2572 mL 5.6430 mL
20 mM 0.1693 mL 0.8465 mL 1.6929 mL 4.2323 mL
25 mM 0.1354 mL 0.6772 mL 1.3543 mL 3.3858 mL
30 mM 0.1129 mL 0.5643 mL 1.1286 mL 2.8215 mL
40 mM 0.0846 mL 0.4232 mL 0.8465 mL 2.1161 mL
50 mM 0.0677 mL 0.3386 mL 0.6772 mL 1.6929 mL
60 mM 0.0564 mL 0.2822 mL 0.5643 mL 1.4108 mL
80 mM 0.0423 mL 0.2116 mL 0.4232 mL 1.0581 mL
100 mM 0.0339 mL 0.1693 mL 0.3386 mL 0.8465 mL
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Nepicastat Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Nepicastat
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HY-13289
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