Home Metabolism Hydroxylase inhibitor (R)-Nepicastat HCl For research use only.

(R)-Nepicastat HCl

Synonyms: RS-25560-198 HCl

(R)-Nepicastat HCl (RS-25560-198), 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.

(R)-Nepicastat HCl Chemical Structure

(R)-Nepicastat HCl Chemical Structure

CAS No. 195881-94-8

Purity & Quality Control

Batch: S492601 DMSO]66 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.26%
99.26

(R)-Nepicastat HCl Related Products

Signaling Pathway

Hydroxylase Signaling Pathways

Hydroxylase Signaling Pathway

Biological Activity

Description (R)-Nepicastat HCl (RS-25560-198), 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
In vitro (R)-Nepicastat produces concentration-dependent inhibition of bovine and human dopamine-β-hydroxylase activity in vitro. [1]
In Vivo
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]
Animal Research Animal Models Animal Models Spontaneously hypertensive rats (SHRs).
Dosages ~30 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 331.81 Formula

C14H15F2N3S.HCl
CAS No. 195881-94-8 SDF --
Smiles C1CC2=C(CC1N3C(=CNC3=S)CN)C=C(C=C2F)F.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 66 mg/mL ( (198.9 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

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.

Handling Instructions

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