| Bioactivity | Fosnetupitant chloride monohydrochloride (Pronetupitant chloride monohydrochloride) is an NK1 antagonist with pKi values of 9.5, 6.1 for human NK1 and NK3 receptor, respectively. Fosnetupitant chloride monohydrochloride is a methylene phosphate prodrug of Netupitant[1]. |
| Invitro | Fosnetupitant chloride monohydrochloride 对 5-HT6 (pKi ∼ 5.2) 受体和 L 型 Ca2+ 通道 (pKi > ∼ 5.7) 表现出微摩尔的亲和力，并且不结合所研究的所有其他蛋白质[1]。 |
| In Vivo | Fosnetupitant chloride monohydrochloride (i.v.) 可以在几分钟内转化为 Netupitant (HY-16346)[1]. |
| Name | Fosnetupitant chloride monohydrochloride |
| CAS | 1643757-72-5 |
| Formula | C31H37Cl2F6N4O5P |
| Molar Mass | 761.52 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 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. |