Fosaprepitant dimeglumine

SKU: orb1307445

Description

Fosaprepitant dimeglumine

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 265121-04-8
• MW: 1004.83
• Purity: 99.03%
• Formula: C₃₇H₅₆F₇N₆O₁₆P
• SMILES: CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.C[C@@H](O[C@H]1OCCN(Cc2nn(c(=O)[nH]2)P(O)(O)=O)[C@H]1c1ccc(F)cc1)c1cc(cc(c1)C(F)(F)F)C(F)(F)F
• Target: Neurokinin receptor
• Solubility: H2O:124 mg/mL (123.4 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:185 mg/mL (184.11 mM)

Bioactivity

• In Vivo:
  Fosaprepitant is converted to aprepitant within 30 min after intravenous administration via the action of ubiquitous phosphatases when administered intravenously. Fosaprepitant is well tolerated up to 150 mg (1 mg/ml), and Fosaprepitant 115 mg is bioequivalent in its AUC to aprepitant 125 mg. Fosaprepitant 115 mg has been submitted for FDA approval as an alternative on day 1 of a 3-day oral aprepitant regimen, with oral aprepitant administered on days 2 and 3.
• In Vitro:
  Fosaprepitant (MK-0517, L-758,298) is a phosphoryl prodrug for aprepitant. Aprepitant is a selective substance P (NK-1 receptor) antagonist approved as part of combination therapy with a corticosteroid and a 5-HT 3 receptor antagonist for the prevention of acute and delayed Chemotherapy-induced nausea and vomiting.

Storage & Handling

• Storage: store at low temperature,keep away from moisture | Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tachykinin receptor, substance-P, vomiting, Fosaprepitant dimeglumine, Fosaprepitant dimeglumine salt, L785298, L-785298, MK 0517, MK0517, MK-0517, nociception, NK1, NK receptor, neuropeptide, Neurokinin Receptor, Neurokinin receptor, Neurokininreceptor, L 785298, antagonist, Aprepitant, chemotherapy-induced

Compound Identifiers

PubChem CID

135564864