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DAAO inhibitor-1

Catalog No. T5206 CAS 2065250-25-9

DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor (IC50: 0.12 μM).

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DAAO inhibitor-1, CAS 2065250-25-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 78.00
5 mg	In stock	$ 183.00
10 mg	In stock	$ 265.00
25 mg	In stock	$ 531.00
50 mg	In stock	$ 768.00
100 mg	In stock	$ 1,070.00

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Purity: 98.51%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor (IC50: 0.12 μM).
Targets&IC50	DAAO:0.12 μM (cell free)
Kinase Assay	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.
Cell Research	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.
Animal Research	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.

Molecular Weight	152.13
Formula	C7H5FN2O
CAS No.	2065250-25-9

Storage

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

Solubility Information

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

References and Literature

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.

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This product is contained In the following compound libraries：

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Keywords

DAAO inhibitor-1 2065250-25-9 Others Inhibitor inhibit DAAO inhibitor 1 DAAO inhibitor1 inhibitor

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