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Chemical Structure| 20205-43-0 Chemical Structure| 20205-43-0

Structure of 6,7-dimethylisatin
CAS No.: 20205-43-0

Chemical Structure| 20205-43-0

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6,7-Dimethylisatin is an MAO (monoamine oxidase) inhibitor with potential research value in depression, Alzheimer's disease, and Parkinson's disease. Additionally, it inhibits hGAT3 (human glycine transporter 3) and also shows inhibitory effects on hBGT1 (human glycine transporter 1) and hGAT2.

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Product Citations

Product Citations

Prinsloo, Izak F. ; Petzer, Jacobus P. ; Cloete, Theunis T. ; Petzer, Anel ;

Abstract: The small mol., isatin, is a well-known reversible inhibitor of the monoamine oxidase (MAO) enzymes with IC50 values of 12.3 and 4.86μM for MAO-A and MAO-B, resp. While the interaction of isatin with MAO-B has been characterized, only a few studies have explored structure-activity relationships (SARs) of MAO inhibition by isatin analogs. The current study therefore evaluated a series of 14 isatin analogs as in vitro inhibitors of human MAO-A and MAO-B. The results indicated good potency MAO inhibition for some isatin analogs with five compounds exhibiting IC50 < 1μM. 4-Chloroisatin (1b) and 5-bromoisatin (1f) were the most potent inhibitors with IC50 values of 0.812 and 0.125μM for MAO-A and MAO-B, resp. These compounds were also found to be competitive inhibitors of MAO-A and MAO-B with Ki values of 0.311 and 0.033μM, resp. Among the SARs, it was interesting to note that C5-substitution was particularly beneficial for MAO-B inhibition. MAO inhibitors are established drugs for the treatment of neuropsychiatric and neurodegenerative disorders, while potential new roles in prostate cancer and cardiovascular disease are being investigated.

Keywords: competitive ; inhibition ; isatin ; monoamine oxidase ; structure-activity relationship

Alternative Products

Product Details of 6,7-dimethylisatin

CAS No. :20205-43-0
Formula : C10H9NO2
M.W : 175.18
SMILES Code : O=C1NC2=C(C=CC(C)=C2C)C1=O
MDL No. :MFCD00047221
InChI Key :GVRLEGBOODEAOX-UHFFFAOYSA-N
Pubchem ID :1810511

Safety of 6,7-dimethylisatin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319
Precautionary Statements:P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313

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Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.71mL

1.14mL

0.57mL

28.54mL

5.71mL

2.85mL

57.08mL

11.42mL

5.71mL

 

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