| 名稱 | DAAO inhibitor-1 |
| 描述 | DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor (IC50: 0.12 μM). |
| 細胞實驗 | Time courses of the unchanged pharmacons in hepatocytes and in hepatic microsomes were obtained. Each compound was incubated with cell suspension (2 × 10^6 cells/mL) or with microsomes (4 mg/mL) at 37 °C in a humid atmosphere containing 5% CO2. The parent compounds were added directly to the cell culture medium or to 0.1 M Tris-HCl buffer (pH 7.4) at the final concentration of 1 μM. The microsomal incubation mixtures contained an NADPH-regenerating system (1 mM NADPH, 10 mM glucose 6–phosphate, 5 mM MgCl2 and 2 units/mL glucose 6-phosphate dehydrogenase). At various time points (at 0, 15, 30, 45, 60, 90, 120, 180, 240 min for hepatocyte incubations; at 0, 15, 30, 45, 60, 90 min for microsomal incubations), the incubation mixtures were sampled (aliquots: 0.25 mL) and terminated by the addition of 0.17 mL ice-cold acetonitrile containing the internal standard, carbamazepine (0.13 μM). The cell and microsomal debris was separated by centrifugation, and the supernatant was analyzed by LC-MS/MS for quantitation of the parent compound. |
| 激酶實驗 | D-2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid (D-kynurenine) was used to measure D-amino acid oxidase activity according to the protocol described in Ref. The measurements were carried out on a Citation3 cell imaging multi-mode microplate reader with 364 well plates. The applied wavelengths were 340 nm and 396 nm. The buffer contained 20 mM TRIS-HCl and 100 mM NaCl. Human DAAO was kept in 1 μg/10 μL aliquots at -80 °C. |
| 動物實驗 | Male NMRI mice of 25–30 g were housed in an air-conditioned (22 +/- 2 °C) animal room with 12 h light and dark cycle. They had free access to standard laboratory rodent chow and water. Five mice per group were treated intraperitoneally with 30 mg/kg D-serine in the absence or presence of 30 mg/kg DAAO inhibitor-1 dissolved in 5% DMSO containing saline. The test compound and D-serine were administered simultaneously. After 10, 20, 30, 60, 120, 240 and 360 min the mice were anesthetized by carbon dioxide, decapitated and their blood was collected using EDTA as anticoagulant. Plasma was obtained by centrifugation at 2000g, 4 °C for 5 min and the samples were stored frozen at -80 °C until analysis. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (26.29 mM), Sonication is recommended.
DMSO : 125 mg/mL (821.67 mM), Sonication is recommended.
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| 關鍵字 | Inhibitor | inhibit | D-amino acid oxidase (DAAO) | DAAO inhibitor-1 | DAAO inhibitor1 | DAAO inhibitor 1 |
| 相關產品 | L-Phenylalanine | Quinolinic acid | L-Glutamic acid | glycine | Memantine | L-Glutamic acid monosodium salt | N-Methylsarcosine | Memantine hydrochloride | Kynurenic acid | Indole-2-carboxylic acid | Decanoic Acid | N,N-Dimethylglycine hydrochloride |
| 相關庫 | 抑制劑庫 | 經典已知活性庫 | 已知活性化合物庫 | 含氟化合物庫 | 神經信號分子庫 | NO PAINS 化合物庫 |