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DAAO inhibitor-1

产品编号 T5206 CAS 2065250-25-9

DAAO inhibitor-1是 D-氨基酸氧化酶抑制剂(IC50:0.12 μM)。

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DAAO inhibitor-1, CAS 2065250-25-9

规格	价格/CNY	货期
1 mg	￥ 688	现货
5 mg	￥ 1,620	现货
10 mg	￥ 2,450	现货
25 mg	￥ 4,130	现货
50 mg	￥ 5,880	现货
100 mg	￥ 8,180	现货

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纯度: 98.51%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor (IC50: 0.12 μM).
靶点活性	DAAO:0.12 μM (cell free)
激酶实验	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.
细胞实验	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.
动物实验	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.

分子量	152.13
分子式	C7H5FN2O
CAS No.	2065250-25-9

存储

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

溶解度

DMSO: 125 mg/mL (821.67 mM), Sonification is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	6.5733 mL	32.8666 mL	65.7333 mL	164.3331 mL
	5 mM	1.3147 mL	6.5733 mL	13.1467 mL	32.8666 mL
	10 mM	0.6573 mL	3.2867 mL	6.5733 mL	16.4333 mL
	20 mM	0.3287 mL	1.6433 mL	3.2867 mL	8.2167 mL
	50 mM	0.1315 mL	0.6573 mL	1.3147 mL	3.2867 mL
	100 mM	0.0657 mL	0.3287 mL	0.6573 mL	1.6433 mL

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参考文献

1. Szilágyi B, et al. Discovery of isatin and 1H-indazol-3-ol derivatives as d-amino acid oxidase (DAAO) inhibitors. Bioorg Med Chem. 2018 May 1;26(8):1579-1587.

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。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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