AS057278

製品コードS5434 バッチS543401

印刷

化学情報

 Chemical Structure Synonyms 3-Methylpyrazole-5-carboxylic acid Storage
(From the date of receipt)
3 years -20°C powder
化学式

C5H6N2O2

分子量 126.11 CAS No. 402-61-9
Solubility (25°C)* 体外 DMSO 25 mg/mL (198.23 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 AS057278 (3-Methylpyrazole-5-carboxylic acid, MPC) is an inhibitor of D-amino acid oxidase (DAAO).
in vitro No inhibitory effect on DASOX were observed with AS057278 at the concentration of 10 μM and no inhibitory effect on serine racemase were observed with AS057278 at the concentration of 50 μM[2].
in vivo MPC is able to increase brain d-serine levels and ameliorate PCP-induced abnormal behavior in SD rat[1]. MPC increaseS D-serine fraction in rat cortex and midbrain (10 mg/kg i.v.). AS057278 was able to normalize phencyclidine (PCP)-induced prepulse inhibition after acute (80 mg/kg) and chronic (20 mg/kg b.i.d.) oral administration in mice. AS057278 after oral chronic treatment (10 mg/kg b.i.d.) was able to normalize PCP-induced hyperlocomotion[2].

プロトコル(参考用のみ)

キナーゼアッセイ DAAO enzymatic assay
Assays were performed in 384 well Corning NBS white plates with clear bottom. Each well contained 5 μL of compound in 10% DMSO or 10% DMSO only, 35 μL DAAO Buffer (FAD 10 μM, Peroxydase 2.63×10-4 UI/μL, O-dianisidine 0.86 mM, BSA 0.1 μg/μL, D-serine 10 mM, Na-pyrophosphate 20 mM pH 9.0 saturated with O2). Reaction was started by the addition of 10 μL DAAO at 30 ng/ μL diluted in Na-pyrophosphate 20 mM pH 9.0 saturated with O2 containing 0.01% BSA. Therefore final concentration of enzyme was 6 ng/μL. Reaction was performed over 40 min at room temperature and was stopped by the addition of 25 μL H2SO4 1 M. Absorbance was measured at 405 nm on a Wallac/Perkin Elmer Victor2V spectrophotometer. Low controls were performed in the absence of enzyme and high controls in the presence of enzyme and vehicle. For determination of IC50 values, assays were performed in triplicate on two independent occasions. The reference compound used was Indol-2 Carboxylic Acid, IC100: 1 μM.
動物実験 動物モデル Male SD rats
投薬量 5.0 or 50 mg/kg
投与方法 i.p.

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。