Bioactivity | Fosnetupitant (Pronetupitant) a methylene phosphate prodrug of Netupitant. Fosnetupitant (Pronetupitant) exhibits a pKi of 9.5 for human NK1 receptor[1]. |
Invitro | Fosnetupitant (Pronetupitant) displays micromolar affinity for the 5-HT6 (pKi ∼ 5.2) receptor and type L Ca2+ channels (pKi ∼ 5.7) and does not bind all the other proteins investigated[1]. |
In Vivo | Pronetupitant is rapidly and extensively converted to Netupitant after i.v. injection in rats[1]. |
Name | Fosnetupitant |
CAS | 1703748-89-3 |
Formula | C31H35F6N4O5P |
Molar Mass | 688.60 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
Reference | [1]. Ruzza C, et al. In vitro and in vivo pharmacological characterization of Pronetupitant, a prodrug of the neurokinin 1 receptor antagonist Netupitant. Peptides. 2015 Jul;69:26-32. |