Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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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.) rapidly metabolizes into Netupitant [1] within minutes. |
Synonyms | Pronetupitant chloride monohydrochloride |
Molecular Weight | 761.52 |
Formula | C31H37Cl2F6N4O5P |
CAS No. | 1643757-72-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Fosnetupitant chloride monohydrochloride 1643757-72-5 GPCR/G Protein Neuroscience Neurokinin receptor Fosnetupitant Chloride Fosnetupitant chloride Monohydrochloride Pronetupitant chloride monohydrochloride Pronetupitant Chloride Pronetupitant chloride Monohydrochloride inhibitor inhibit