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Fosnetupitant chloride monohydrochloride

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

Fosnetupitant chloride monohydrochloride

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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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.
AliasPronetupitant chloride monohydrochloride
Chemical Properties
Molecular Weight761.52
FormulaC31H37Cl2F6N4O5P
Cas No.1643757-72-5
Storage & Solubility Information
StorageShipping with blue ice.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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