Fosaprepitant dimeglumine salt (Synonyms: MK 0517) |
رقم الكتالوجGC10659 |
يعتبر ملح ديمجلومين فوسابريتانت (MK-0517) دواءً أوليًا لـ Aprepitant.
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Cas No.: 265121-04-8
Sample solution is provided at 25 µL, 10mM.
Fosaprepitant dimeglumine salt (L-758,298 MK-0517) is an antagonist of neurokinin-1[1].
Fosaprepitant dimeglumine salt has shown the pharmacodynamic function by its active metabolite aprepitant. Fosaprepitanot dimeglumine salt has been found to be a highly selective antagonist of the NK-1 receptor and inhibit the cation of substance P. In addition, Fosaprepitant dimeglumine salt has been exhibited to have the effect on cisplatin induced emesis in the classical ferret model. Besides, because of the brain penetrating of aprepitant, Fosaprepitant dimeglumine salt has been revealed to have a very high affinity for the NK-1 receptor and increase the efficacy by dexamethasone, granisetron and so on. Fosaprepitant dimeglumine salt has been evaluated to use in the prevention of chemotherapy-induced nausea and vomiting (CINV) by combination with a 5-HT3 antagonist and a steroid [1].
References:
[1] Van Belle SJ1, Cocquyt V. Fosaprepitant dimeglumine (MK-0517 or L-785,298), an intravenous neurokinin-1 antagonist for the prevention of chemotherapy induced nausea and vomiting.Expert Opin Pharmacother. 2008 Dec; 9(18):3261-70.
Cas No. | 265121-04-8 | SDF | |
المرادفات | MK 0517 | ||
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;(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol | ||
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.CNCC(C(C(C(CO)O)O)O)O.CNCC(C(C(C(CO)O)O)O)O | ||
Formula | C37H56F7N6O16P | M.Wt | 1004.83 |
الذوبان | ≥ 50.2415mg/mL in DMSO | Storage | Store at -20°C,unstable in solution, ready to use. |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 0.9952 mL | 4.976 mL | 9.9519 mL |
5 mM | 0.199 mL | 0.9952 mL | 1.9904 mL |
10 mM | 0.0995 mL | 0.4976 mL | 0.9952 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
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