Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Fosaprepitant dimeglumine 是 Aprepitant 的前药。它是一种神经激肽 1 受体拮抗剂，可用于预防化疗引起的恶心呕吐。
| 产品描述 | Fosaprepitant Dimeglumine is the dimeglumine salt form of fosaprepitant, the water-soluble, N-phosphorylated prodrug of aprepitant, with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent binds selectively to the human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS). This inhibits receptor binding of the endogenous substance P and prevents substance P-induced emesis. |
| 体外活性 | 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. [1] |
| 体内活性 | 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. [1] |
| 激酶实验 | Biochemical Methods: EPZ-6438 is incubated for 30 min with 40 μL per well of 5 nM PRC2 (final assay concentration in 50 μL is 4 nM ) in 1X assay buffer (20 mM Bicine [pH 7.6], 0.002% Tween-20, 0.005% Bovine Skin Gelatin and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer 3 H-SAM, unlabeled SAM, and peptide representing histone H3 residues 21-44 containing C-terminal biotin (appended to a C-terminal amide-capped lysine) are added to initiate the reaction (both substrates are present in the final reaction mixture at their respective Km values, an assay format referred to as ‘‘balanced conditions''. The final concentrations of substrates and methylation state of the substrate peptide are indicated for each enzyme Reactions are incubated for 90 min at room temperature and quenched with 10 μL per well of 600 μM unlabeled SAM, Then transferred to a 384-well flashplate and washed after 30 min. |
| 别名 | 福沙匹坦二甲葡胺, MK-0517, 福沙吡坦二甲葡胺, Fosaprepitant dimeglumine salt, L785298 |
| 分子量 | 1004.83 |
| 分子式 | C37H56F7N6O16P |
| CAS No. | 265121-04-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 185 mg/mL (184.1 mM)
Ethanol: <1 mg/mL
H2O: 124 mg/mL (123.4 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
参考文献
剂量换算对于不同动物的给药剂量换算，您也可以参考 更多...
体内实验配液计算器请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法： 比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)， 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。
体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300， 混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。
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您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。
Fosaprepitant dimeglumine 265121-04-8 GPCR/G Protein Neuroscience Neurokinin receptor nociception NK receptor MK 0517 antagonist 福沙匹坦二甲葡胺 MK-0517 Aprepitant Inhibitor receptor 福沙吡坦二甲葡胺 chemotherapy-induced L 785298 nausea Tachykinin receptor Fosaprepitant dimeglumine salt L-785298 substance-P L785298 inhibit MK0517 Neurokinin Receptor vomiting neuropeptide inhibitor
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