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DAAO inhibitor-1

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Catalog No. T5206Cas No. 2065250-25-9

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

DAAO inhibitor-1

DAAO inhibitor-1

🥰Excellent
Purity: 98.51%
Catalog No. T5206Cas No. 2065250-25-9
DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor with an IC50 of 0.12 μM.
Pack SizePriceAvailabilityQuantity
1 mg$47In Stock
5 mg$110In Stock
10 mg$159In Stock
25 mg$319In Stock
50 mg$461In Stock
100 mg$642In Stock
200 mg$865In Stock
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Purity:98.51%
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Product Introduction

Bioactivity
Description
DAAO inhibitor-1 is a potent D-amino acid oxidase (DAAO) inhibitor with an IC50 of 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.
Chemical Properties
Molecular Weight152.13
FormulaC7H5FN2O
Cas No.2065250-25-9
SmilesOC1=C2C(=NN1)C=C(F)C=C2
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 125 mg/mL (821.67 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM6.5733 mL32.8666 mL65.7333 mL328.6663 mL
5 mM1.3147 mL6.5733 mL13.1467 mL65.7333 mL
10 mM0.6573 mL3.2867 mL6.5733 mL32.8666 mL
20 mM0.3287 mL1.6433 mL3.2867 mL16.4333 mL
50 mM0.1315 mL0.6573 mL1.3147 mL6.5733 mL
100 mM0.0657 mL0.3287 mL0.6573 mL3.2867 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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