(R)-Nepicastat HCl

Catalog No.S4926 Synonyms: RS-25560-198 HCl

(R)-Nepicastat HCl Chemical Structure

Molecular Weight(MW): 331.81

(R)-Nepicastat 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.

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Biological Activity

Description (R)-Nepicastat 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.
Targets
Human dopamine-beta-hydroxylase [1] Bovine dopamine-beta-hydroxylase [1]
18.3 nM 25.1 nM
In vitro

(R)-Nepicastat produces concentration-dependent inhibition of bovine and human dopamine-β-hydroxylase activity in vitro. [1]

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). [1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Animal Models Spontaneously hypertensive rats (SHRs).
  • Formulation: Distilled water
  • Dosages: ~30 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (198.9 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 331.81
Formula

C14H15F2N3S.HCl

CAS No. 195881-94-8
Storage powder
in solvent
Synonyms RS-25560-198 HCl

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Hydroxylase Signaling Pathway Map

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