Nepicastat
Based on 3 publication(s) in Google Scholar
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).
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- CAS No.: 173997-05-2
- Formule: C14H15F2N3S
- Masse moléculaire:295.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Nepicastat
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Activité biologique
IC50: 8.5 nM (bovine dopamine-beta-hydroxylase), 9 nM (human dopamine-beta-hydroxylase)[2]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:15-16 weeks male spontaneously hypertensive rats (SHRs)[3]
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Dosage:Oral administration; three consecutive times, 12 hours apart
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Administration:3, 10, 30, 100 mg/kg
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 173997-05-2
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Masse moléculaire 295.35
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Formule C14H15F2N3S
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SMILES
FC1=CC(F)=C2CC[C@@H](CC2=C1)N3C(CN)=CNC3=S
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Synonyms
SYN117; RS-25560-197
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
The sympathetic nervous system drives hyperinflammatory responses to Clostridioides difficile infection. [Abstract]2024 Oct 1:101771. PMID: 39368481 -
Commun Biol
2022 Jan 25;5(1):96. PMID: 35079095 -
Solvant et solubilité
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
Références
[1]. Beliaev A, et al. Synthesis and biological evaluation of novel, peripherally selective chromanyl imidazolethione-based inhibitors of dopamine beta-hydroxylase.J Med Chem. 2006 Feb 9;49(3):1191-7. [Content Brief]
[2]. Stanley WC, et al. Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of dopamine-beta-hydroxylase.Br J Pharmacol. 1997 Aug;121(8):1803-9. [Content Brief]
[3]. Stanley WC, et al. Cardiovascular effects of nepicastat (RS-25560-197), a novel dopamine beta-hydroxylase inhibitor. J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70. [Content Brief]
[4]. Sabbah HN, et al. Effects of dopamine beta-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. [Content Brief]
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 |
Nepicastat Related Classifications
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