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(R)-Nepicastat HCl

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Catalog No. T6356Cas No. 195881-94-8
Alias RS-25560-198 HCl

(R)-Nepicastat HCl (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.

(R)-Nepicastat HCl

(R)-Nepicastat HCl

😃Good
Catalog No. T6356Alias RS-25560-198 HClCas No. 195881-94-8
(R)-Nepicastat HCl (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.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$1356-8 weeks6-8 weeks
10 mg$2296-8 weeks6-8 weeks
25 mg$4326-8 weeks6-8 weeks
50 mg$5856-8 weeks6-8 weeks
100 mg$8556-8 weeks6-8 weeks
1 mL x 10 mM (in DMSO)$1356-8 weeks6-8 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
(R)-Nepicastat HCl (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.
Targets&IC50
DBH (bovine):25.1 nM, DBH (human):18.3 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]
SynonymsRS-25560-198 HCl
Chemical Properties
Molecular Weight331.81
FormulaC14H15F2N3S·HCl
Cas No.195881-94-8
SmilesCl.NCC1=CNC(=S)N1[C@@H]1CCC2=C(F)C=C(F)C=C2C1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: <1 mg/mL
DMSO: 61 mg/mL (183.84 mM), Sonication is recommended.
Ethanol: <1 mg/mL
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.0138 mL15.0689 mL30.1377 mL150.6886 mL
5 mM0.6028 mL3.0138 mL6.0275 mL30.1377 mL
10 mM0.3014 mL1.5069 mL3.0138 mL15.0689 mL
20 mM0.1507 mL0.7534 mL1.5069 mL7.5344 mL
50 mM0.0603 mL0.3014 mL0.6028 mL3.0138 mL
100 mM0.0301 mL0.1507 mL0.3014 mL1.5069 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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