Fosaprepitant
Fosaprepitant (CAS 172673-20-0), also known as MK-0517 or L-758,298, is a selective neurokinin-1 (NK-1) receptor antagonist exerting its pharmacological effects primarily through its active metabolite, aprepitant. This antagonism blocks substance P-mediated biological effects, including vomiting responses. In established preclinical models such as the cisplatin-triggered emesis in ferrets, fosaprepitant demonstrated activity in mitigating chemotherapy-induced vomiting. Given aprepitant's favorable penetration into the central nervous system, fosaprepitant exhibits high NK-1 receptor affinity and potentiates antiemetic actions of agents such as dexamethasone and granisetron. It is used in combination therapies with 5-HT3 antagonists and corticosteroids for chemotherapy-induced nausea and vomiting (CINV).
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 614.41 |
| Cas No. | 172673-20-0 |
| Formula | C23H22F7N4O6P |
| Solubility | ≥30.5 mg/mL in DMSO; insoluble in H2O; ≥22.13 mg/mL in EtOH with ultrasonic |
| Chemical Name | [5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-3-oxo-1H-1,2,4-triazol-2-yl]phosphonic acid |
| SDF | Download SDF |
| Canonical SMILES | CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OC2C(N(CCO2)CC3=NC(=O)N(N3)P(=O)(O)O)C4=CC=C(C=C4)F |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
