Fosaprepitant dimeglumine saltNeurokinin-1 antagonist CAS# 265121-04-8 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 265121-04-8 | SDF | Download SDF |
| PubChem ID | 15527165 | Appearance | Powder |
| Formula | C37H56F7N6O16P | M.Wt | 1004.83 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | MK-0517 | ||
| Solubility | H2O : 50 mg/mL (49.76 mM; Need 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;(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol | ||
| 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 | ||
| Standard InChIKey | VRQHBYGYXDWZDL-OOZCZQCLSA-N | ||
| Standard InChI | InChI=1S/C23H22F7N4O6P.2C7H17NO5/c1-12(14-8-15(22(25,26)27)10-16(9-14)23(28,29)30)40-20-19(13-2-4-17(24)5-3-13)33(6-7-39-20)11-18-31-21(35)34(32-18)41(36,37)38;2*1-8-2-4(10)6(12)7(13)5(11)3-9/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H,31,32,35)(H2,36,37,38);2*4-13H,2-3H2,1H3/t12-,19+,20-;2*4-,5+,6+,7+/m100/s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Fosaprepitant dimeglumine(MK-0517) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting.
IC50 Value:
Target: NK1 receptor
in vitro: Fosaprepitant (also known as MK-0517 and L-758,298) is a water-soluble phosphoryl prodrug for aprepitant, which, when administered intravenously, is converted to aprepitant within 30 min of intravenous administration via the action of ubiquitous phosphatases. Owing to the rapid conversion offosaprepitant to the active form (aprepitant), fosaprepitant 115 mg provided the same aprepitant exposure in terms of AUC as aprepitant 12 mg orally, and fosaprepitant is expected to provide a correspondingly similar antiemetic effect as aprepitant [1].
in vivo: Fosaprepitant is well tolerated with mild to moderate venous irritation being the only additional toxicity to those seen with oral aprepitant, and that is a function of dose, concentration, and infusion rate [2]. Patients receiving cisplatin ≥ 70 mg/m(2) for the first time received ondansetron and dexamethasone with a standard aprepitant regimen (125 mg on day 1, 80 mg on day 2, 80 mg on day 3) or a single-dose fosaprepitant regimen (150 mg on day 1) [3]. Single-dose fosaprepitant used in combination with granisetron and dexamethasone was well-tolerated and effective in preventing chemotherapy-induced nausea and vomiting in patients receiving highly emetogenic cancer chemotherapy, including high-dose cisplatin [4]. References: | |||||
Fosaprepitant dimeglumine salt Dilution Calculator
Fosaprepitant dimeglumine salt Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 0.9952 mL | 4.976 mL | 9.9519 mL | 19.9039 mL | 24.8798 mL |
| 5 mM | 0.199 mL | 0.9952 mL | 1.9904 mL | 3.9808 mL | 4.976 mL |
| 10 mM | 0.0995 mL | 0.4976 mL | 0.9952 mL | 1.9904 mL | 2.488 mL |
| 50 mM | 0.0199 mL | 0.0995 mL | 0.199 mL | 0.3981 mL | 0.4976 mL |
| 100 mM | 0.01 mL | 0.0498 mL | 0.0995 mL | 0.199 mL | 0.2488 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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