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 | (3-(((2R,3S)-2-(1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(4-fluorophenyl)morpholino)methyl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-1-yl)phosphonic acid |
| SDF | Download SDF |
| Canonical SMILES | C(N1[C@H]([C@@H](O[C@H](C)C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)OCC1)C3=CC=C(F)C=C3)C4=NN(P(=O)(O)O)C(=O)N4 |
| 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
