product name (R)-Nepicastat HCl
Description: (R)-Nepicastat HCl (also known as RS-25560-198 HCl), the R-enantiomer of Nepicastat HCl, is a potent and selective inhibitor with IC50 of 25.1 nM and 18.3 nM for bovine and human dopamine-β-hydroxylase, with negligible affinity for twelve other enzymes and thirteen neurotransmitter receptors. Nepicastat has been studied as a possible treatment for congestive heart failure, and appears to be well tolerated.
References: Br J Pharmacol. 1997 Aug;121(8):1803-9.
331.81
Formula
C14H15F2N3S.HCl
CAS No.
195881-94-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 66 mg/mL (198.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
RS-25560-198 HCl
other peoduct :
| In Vitro |
In vitro activity: (R)-Nepicastat produces concentration-dependent inhibition of bovine and human dopamine-β-hydroxylase activity in vitro. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | (R)-Nepicastat (30 mg/kg, p.o.) reduces noradrenaline content, dopamine content and dopamine/noradrenaline ratio in mesenteric artery and left ventricle of spontaneously hypertensive rats (SHRs). |
| Animal model | Animal Models Spontaneously hypertensive rats (SHRs). |
| Formulation & Dosage | Dissolved in distilled water; 30 mg/kg; p.o. |
| References | Br J Pharmacol. 1997 Aug;121(8):1803-9. |
