(R)-Nepicastat HCl

Catalog No.S4926

(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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(R)-Nepicastat HCl Chemical Structure

(R)-Nepicastat HCl Chemical Structure
Molecular Weight: 331.81

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Product Information

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Product Description

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]
IC50 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(Only for Reference)

Kinase Assay: [1]

In vitro studies Bovine and human dopamine-beta-hydroxylase activity are assayed by measuring the conversion of tyramine to octopamine. Human dopamine-beta-hydroxylase is purified from the culture medium of the neuroblastoma cell line SK-N-SH. The assay is performed at pH 5.2 and 32°C in a medium containing 0.125 M sodium acetate, 10 mM fumarate, 0.5 ± 2 μM CuSO4, 0.1 mg/mL catalase, 0.1 mM tyramine and 4 mM ascorbate. In a typical assay, 0.5 ± 1 mu of enzyme are added to the reaction mixture and, subsequently, a substrate mixture containing catalase, tyramine and ascorbate is added to initiate the reaction (final volume of 0.2 mL). Samples are incubated with or without the appropriate concentration of nepicastat (RS-25560-197, S-enantiomer) or RS-25560-198 (R-enantiomer) at 37 °C for 30-40 minutes. The reaction is quenched by the stop solution containing 25 mM EDTA and 240 μM 3-hydroxytyramine (internal standard). The samples are analysed for octopamine by reverse phase high pressure liquid chromatography (h.p.l.c.) with ultraviolet (u.v.)-detection at 280 nM. The h.p.l.c. run is carried out at a flow rate of 1 mL/min with a LiChroCART 125-4 RP-18 column and isocratic elution with 10 mM acetic acid, 10 mM 1-heptane sulphonic acid, 12 mM tetrabutyl ammonium phosphate and 10% methanol. The remaining % activity is calculated based on controls (without RS 25560), corrected with internal standards and fitted to a non-linear four-parameter concentration-response curve. The activity of nepicastat at twelve selected enzymes and receptors is determined by use of established assays. Binding data are analysed by iterative curve-fitting to a four parameter logistic equation. Ki values are calculated from IC50 values by the Cheng-Pruso€ equation. Enzyme inhibitory activity is expressed as IC50 (concentration required to produce 50% inhibition of enzyme activity).

Animal Study: [1]

Animal Models Animal Models Spontaneously hypertensive rats (SHRs).
Formulation Distilled water
Dosages ~30 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Stanley WC, et al. Br J Pharmacol. 1997, 121(8), 1803-1809.

Chemical Information

Molecular Weight (MW) 331.81


CAS No. 195881-94-8
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms RS-25560-198 HCl
Solubility (25°C) * In vitro DMSO 66 mg/mL (198.9 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name 2H-​Imidazole-​2-​thione, 5-​(aminomethyl)​-​1-​[(2R)​-​5,​7-​difluoro-​1,​2,​3,​4-​tetrahydro-​2-​naphthalenyl]​-​1,​3-​dihydro-​, hydrochloride (1:1)

Tech Support

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