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Nepicastat

Chemical Structure : Nepicastat

CAS No.: 173997-05-2

Nepicastat (SYN117;RS-25560-197;SYN-117;SYN 117)

Catalog No.: PC-43466Not For Human Use, Lab Use Only.

Nepicastat (RS-25560-197, SYN-117) is a potent, selective, orally active inhibitor of dopamine-beta-hydroxylase (DBH) with IC50 of 8.5 and 9.0 nM for bovine and human DBH, respectively.

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Biological Activity

Nepicastat (RS-25560-197, SYN-117) is a potent, selective, orally active inhibitor of dopamine-beta-hydroxylase (DBH) with IC50 of 8.5 and 9.0 nM for bovine and human DBH, respectively; Nepicastat is 2-3 fold more potent than the corresponding R-enantiomer (RS-25560-198); produces dose-dependent decreases in noradrenaline content, increases in dopamine content and increases in dopamine/noradrenaline ratio in the artery, left ventricle and cerebral cortex in spontaneously hypertensive rats.

Hypertension

Discontinued

Physicochemical Properties

M.Wt
Formula C14H15F2N3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 48 mg/mL

Chemical Name/SMILES

2H-Imidazole-2-thione, 5-(aminomethyl)-1-[(2S)-5,7-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]-1,3-dihydro-

References

1. Stanley WC, et al. Br J Pharmacol. 1997 Aug;121(8):1803-9.

2. Stanley WC, et al. J Cardiovasc Pharmacol. 1998 Jun;31(6):963-70.

3. Sabbah HN, et al. Circulation. 2000 Oct 17;102(16):1990-5.

4. Schroeder JP, et al. Neuropsychopharmacology. 2010 Nov;35(12):2440-9.

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