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Submit ReviewNepicastat hydrochloride
Description: Potent and selective dopamine β-hydroxylase (DBH) inhibitor; orally bioavailable
Chemical Name: 5-(Aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-2H-imidazole-2-thione hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for Nepicastat hydrochloride
Nepicastat hydrochloride is a potent and selective dopamine β-hydroxylase (DBH) inhibitor (IC50 = 9 nM). Selective for DBH over 12 other enzymes. Decreases noradrenaline and increases dopamine levels in tissues and plasma in hypertensive rats. Prevents progressive left ventricular dysfunction in an in vivo heart failure model. Also potentiates the stimulus effects of cocaine without producing cocaine-like effects in rats. Orally bioavailable.
Technical Data for Nepicastat hydrochloride
| M. Wt | 331.81 |
| Formula | C14H15F2N3S.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 170151-24-3 |
| PubChem ID | 9840545 |
| InChI Key | DIPDUAJWNBEVOY-PPHPATTJSA-N |
| Smiles | S=C(NC=C3CN)N3[C@H]2CCC1=C(F)C=C(F)C=C1C2.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Nepicastat hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 33.18 | 100 |
Preparing Stock Solutions for Nepicastat hydrochloride
The following data is based on the product molecular weight 331.81. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.01 mL | 15.07 mL | 30.14 mL |
| 5 mM | 0.6 mL | 3.01 mL | 6.03 mL |
| 10 mM | 0.3 mL | 1.51 mL | 3.01 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
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Product Datasheets for Nepicastat hydrochloride
References for Nepicastat hydrochloride
References are publications that support the biological activity of the product.
Manvich et al (2013) DA β-hydroxylase inhibitors enhance the discriminative stimulus effects of cocaine in rats. J.Pharmacol.Exp.Ther. 347 564 PMID: 24068832
Sabbah et al (2000) Effects of DA β-hydroxylase inhibition with nepicastat on the progression of left ventricular dysfunction and remodeling in dogs with chronic heart failure. Circulation 102 1990 PMID: 11034950
Stanley et al (1997) Catecholamine modulatory effects of nepicastat (RS-25560-197), a novel, potent and selective inhibitor of DA-beta-hydroxylase. Br.J.Pharmacol. 121 1803 PMID: 9283721
If you know of a relevant reference for Nepicastat hydrochloride, please let us know.
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Keywords: Nepicastat hydrochloride, Nepicastat hydrochloride supplier, dopamine, beta-hydroxylase, inhibitors, inhibits, β, B-hydroxylase, DBH, noradrenaline, norepinephrine, potent, selective, orally, bioavailable, Hydroxylases, 5037, Tocris Bioscience
1 Citation for Nepicastat hydrochloride
Citations are publications that use Tocris products. Selected citations for Nepicastat hydrochloride include:
Armando et al (2021) Synergistic Growth Inhibition of HT-29 Colon and MCF-7 Breast Cancer Cells with Simultaneous and Sequential Combinations of Antineoplastics and CNS Drugs. Int J Mol Sci 22 PMID: 34299028
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