AS057278

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Chemical Structure| 402-61-9 同义名 : 3-Methylpyrazole-5-carboxylic acid
CAS号 : 402-61-9
货号 : A346208
分子式 : C5H6N2O2
纯度 : 97%
分子量 : 126.11
MDL号 : MFCD00090754
存储条件：

Pure form Keep in dark place, sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(832.58 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 AS057278, a potent in vitro (IC50=0.91 mM) and ex vivo (ED50=2.2-3.95 mM) DAAO inhibitor, was able to increase 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]. Pretreatment with AS057278 significantly suppressed the DA release induced by d-Trp[3]. The effect of insulin in restoration of PDHP phosphatase activity of starved rats was not mimicked by AS057278[4]. Rats made tolerant to nicotinic acid also became tolerant to both AS057278 and to pyridyl-3-tetrazole and rats made tolerant to these antilipolytic agents were also tolerant to nicotinic acid[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

7.93mL

1.59mL

0.79mL

39.65mL

7.93mL

3.96mL

79.30mL

15.86mL

7.93mL
参考文献

[2]Adage T, Trillat AC, Quattropani A, Perrin D, Cavarec L, Shaw J, Guerassimenko O, Giachetti C, Gréco B, Chumakov I, Halazy S, Roach A, Zaratin P. In vitro and in vivo pharmacological profile of AS057278, a selective d-amino acid oxidase inhibitor with potential anti-psychotic properties. Eur Neuropsychopharmacol. 2008 Mar;18(3):200-14

[3]Yoshihara S, Otani H, Tsunoda M, Ishii K, Iizuka H, Ichiba H, Fukushima T. Alterations in extracellular tryptophan and dopamine concentrations in rat striatum following peripheral administration of D- and L-tryptophan: an in vivo microdialysis study. Neurosci Lett. 2012 Sep 20;526(1):74-8

[4]Cockburn BN, Coore HG. Starvation reduces pyruvate dehydrogenase phosphate phosphatase activity in rat kidney. Mol Cell Biochem. 1995 Aug-Sep;149-150:131-6

[5]Myles DD, Stratton GD, Strong P, Skidmore IF. The development of tolerance to antilipolytic agents in rats. Biochem Pharmacol. 1985 Jan 15;34(2):269-74