Isatin

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Chemical Structure| 91-56-5 同义名 : 吲哚-2,3-二酮 ;Indoline-2,3-dione
CAS号 : 91-56-5
货号 : A117648
分子式 : C8H5NO2
纯度 : 98%
分子量 : 147.131
MDL号 : MFCD00005718
存储条件：

Pure form 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(713.65 mM)，配合低频超声助溶，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：

IP 5%DMSO + 2%tween80 +30%PEG400 + water 10 mg/mL clear

生物活性
靶点

  • MAO

    MAO, IC50:15 μM

  • MAO-B

    MAO-B, IC50:14 μM

  • MAO-A

    MAO-A, IC50:58 μM
描述 Isatin (Indoline-2,3-dione) is a potent inhibitor of monoamine oxidase (MAO) with an IC50 of 3 μM, also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 μM)[3]. Isatin is an endogenous indole that is increased in stress, inhibits monoamine oxidase (MAO) B and improves bradykinesia and striatal dopamine levels in rat models of Parkinson's disease. In dopaminergic SH-SY5Y cells (human neuroblastoma) isatin (1-400 μM) induces cell death in dose- and time dependent manner. This death occurred as a continuum of survival, apoptosis and necrosis[4]. A single dose of isatin (80 mg/kg) has a rapid effect on the serotonergic system in the hypothalamus. Isatin significantly increases 5-HT concentrations in the hypothalamus and cortex but did not significantly alter 5-HIAA concentrations[5]. Isatin concentration in blood can exceed 1 mM and tissue concentrations vary from < 0.1 to 10 mM. Its level in the brain and periphery is increased by stress. Isatin has a wide spectrum of behavioural and metabolic effects. It is anxiogenic at lower doses and sedative at higher doses. Its most potent known in vitro actions are as an antagonist of atrial natriuretic peptide (ANP) function and NO signaling[6]. At doses of 100 mg/kg and above, isatin is neuroprotective in different experimental models of neurodegeneration[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

6.80mL

1.36mL

0.68mL

33.98mL

6.80mL

3.40mL

67.97mL

13.59mL

6.80mL
参考文献

[1]Igosheva N, Lorz C, et al. Isatin, an endogenous monoamine oxidase inhibitor, triggers a dose- and time-dependent switch from apoptosis to necrosis in human neuroblastoma cells. Neurochem Int. 2005 Aug;47(3):216-24.

[2]Hamaue N, Minami M, et al. Comparative study of the effects of isatin, an endogenous MAO-inhibitor, and selegiline on bradykinesia and dopamine levels in a rat model of Parkinson's disease induced by the Japanese encephalitis virus. Neurotoxicology. 2004 Jan;25(1-2):205-13.

[3]Isatin: Identity with the Purified Endogenous Monoamine Oxidase Inhibitor Tribulin

[4]Igosheva N, Lorz C, O'Conner E, Glover V, Mehmet H. Isatin, an endogenous monoamine oxidase inhibitor, triggers a dose- and time-dependent switch from apoptosis to necrosis in human neuroblastoma cells. Neurochem Int. 2005 Aug;47(3):216-24

[5]McIntyre IM, Norman TR. Serotonergic effects of isatin: an endogenous MAO inhibitor related to tribulin. J Neural Transm Gen Sect. 1990;79(1-2):35-40

[6]Medvedev A, Igosheva N, Crumeyrolle-Arias M, Glover V. Isatin: role in stress and anxiety. Stress. 2005 Sep;8(3):175-83

[7]Medvedev A, Kopylov A, Buneeva O, Kurbatov L, Tikhonova O, Ivanov A, Zgoda V. A Neuroprotective Dose of Isatin Causes Multilevel Changes Involving the Brain Proteome: Prospects for Further Research. Int J Mol Sci. 2020 Jun 11;21(11):4187