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Fosnetupitant chloride monohydrochloride

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Catalog No. T78104Cas No. 1643757-72-5
Alias Pronetupitant chloride monohydrochloride

Fosnetupitant chloride monohydrochloride (Pro-netupitant chloride monohydrochloride) is a selective NK1 antagonist exhibiting high affinity for the human NK1 receptor with a pK i value of 9.5, and a lower affinity for the NK3 receptor with a pK i of 6.1. It serves as a methylene phosphate prodrug of Netupitant [1].

Fosnetupitant chloride monohydrochloride
Other Forms of Fosnetupitant chloride monohydrochloride:
FosnetupitantT153411703748-89-3
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Fosnetupitant chloride monohydrochloride

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Catalog No. T78104Alias Pronetupitant chloride monohydrochlorideCas No. 1643757-72-5
Fosnetupitant chloride monohydrochloride (Pro-netupitant chloride monohydrochloride) is a selective NK1 antagonist exhibiting high affinity for the human NK1 receptor with a pK i value of 9.5, and a lower affinity for the NK3 receptor with a pK i of 6.1. It serves as a methylene phosphate prodrug of Netupitant [1].
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50 mgInquiry8-10 weeks8-10 weeks
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Product Introduction

Bioactivity
Description
Fosnetupitant chloride monohydrochloride (Pro-netupitant chloride monohydrochloride) is a selective NK1 antagonist exhibiting high affinity for the human NK1 receptor with a pK i value of 9.5, and a lower affinity for the NK3 receptor with a pK i of 6.1. It serves as a methylene phosphate prodrug of Netupitant [1].
Targets&IC50
NK1 (human):9.5 (pKi), NK3 (human):6.1 (pKi)
In vitro
Fosnetupitant chloride monohydrochloride demonstrates micromolar affinity for 5-HT6 receptors (pKi ∼ 5.2) and L-type Ca2+ channels (pKi > ∼ 5.7), without binding to any other proteins studied [1].
In vivo
Fosnetupitant chloride monohydrochloride (i.v.) quickly metabolizes into Netupitant [1] within minutes.
SynonymsPronetupitant chloride monohydrochloride
Chemical Properties
Molecular Weight761.52
FormulaC31H37Cl2F6N4O5P
Cas No.1643757-72-5
SmilesO=C(C(C)(C)C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)N(C)C2=CN=C(N3CC[N+](COP(O)(O)=O)(CC3)C)C=C2C4=C(C)C=CC=C4.[Cl-].Cl
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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:
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2 Enter the in vivo formulation:
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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

Pronetupitant chloride MonohydrochloridePronetupitant ChlorideNeurokininreceptorNeurokinin receptorFosnetupitant chloride MonohydrochlorideFosnetupitant Chloride
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