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Netupitant competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). Recent mechanistic studies using NG108-15 cells have shown that palonosetron and netupitant, an NK1 receptor antagonist currently in phase 3 clinical trials, exhibited synergistic effects when inhibiting the substance P response.The present studies showed that both netupitant and palonosetron-induced NK1 receptor internalization in NG108-15 cells and that when used together receptor internalization was additive.Netupitant was well tolerated with most treatment emergent adverse events (AEs) being mild.Palonosetron and netupitant, either alone or in combination, were effective in reducing the induced elevated pPKA levels during the delayed phase.
| Molecular Weight | 578.59 |
| Formula | C30H32F6N4O |
| CAS Number | 290297-26-6 |
| Solubility (25°C) | DMSO 6 mg/mL heat to 50°C and ultrasonic |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Neurokinin Receptor Products |
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| Aprepitant
Aprepitant (Emend) is an antiemetic chemical compound that belongs to a class of compounds called substance P antagonists (SPA). |
| Maropitant
Maropitant (Cerenia) is a novel, selective neurokinin type-1 (NK1) receptor antagonist. |
| Eprazinone dihydrochloride
Eprazinone is a mucolytic. |
| Fosaprepitant dimeglumine salt
Fosaprepitant is a water-soluble phosphoryl procompound for Aprepitant which is a NK1 antagonist.*The compound is unstable in solutions, freshly prepared is recommended |
| Monohydroxy Netupitant
Monohydroxy Netupitant is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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