福沙吡坦二甲葡胺 T1790

Product Introduction
Bioactivity


英文名: Fosaprepitant dimeglumine

描述: Fosaprepitant dimeglumine (MK-0517) 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。

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.

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 185 mg/mL (184.1 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 124 mg/mL (123.4 mM)


关键字: nociception | NK receptor | MK0517 | antagonist | Aprepitant | Inhibitor | receptor | chemotherapy-induced | L-785298 | nausea | Tachykinin receptor | substance-P | inhibit | Neurokinin Receptor | vomiting | neuropeptide | L 785298 | Fosaprepitant dimeglumine | MK 0517

相关产品: Hemokinin 1 (mouse) acetate(208041-90-1 free base) | Vofopitant dihydrochloride | Casopitant mesylate | Eledoisin | Eprazinone dihydrochloride | Neurokinin A(4-10) TFA(97559-35-8 free base) | Tradipitant | Maropitant citrate | Lanepitant 2HCl | NK3R-IN-1

相关库: Drug Repurposing Compound Library | Approved Drug Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Obesity Compound Library | Anti-Cancer Approved Drug Library | NO PAINS Compound Library

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