858515-82-9

Usage

Uses

Used in Pharmaceutical Industry:
1-(CyclohexylMethyl)-1H-indole-3-carboxylic Acid Methyl Ester is used as a potent and selective inhibitor of mast cell tryptase for its ability to modulate the activity of this enzyme, which plays a crucial role in various physiological and pathological processes. Its excellent selectivity against other serine proteases makes it a valuable candidate for the development of targeted therapies in conditions where mast cell tryptase activity is implicated, such as inflammatory disorders and certain types of cancer.
Used in Drug Development:
In the drug development sector, 1-(CyclohexylMethyl)-1H-indole-3-carboxylic Acid Methyl Ester serves as a lead compound for the design and synthesis of new drugs targeting mast cell tryptase. Its unique structure and inhibitory properties can be further optimized to improve potency, selectivity, and pharmacokinetic properties, leading to the development of more effective and safer medications for the treatment of diseases associated with mast cell tryptase dysregulation.
Used in Research Applications:
1-(CyclohexylMethyl)-1H-indole-3-carboxylic Acid Methyl Ester is also used as a research tool in the study of mast cell tryptase function and its role in various biological processes. It can be employed in in vitro and in vivo experiments to investigate the effects of mast cell tryptase inhibition on cellular signaling pathways, immune responses, and disease progression. This knowledge can contribute to a better understanding of the underlying mechanisms of mast cell tryptase-related diseases and aid in the identification of novel therapeutic targets.

Upstream product

• 942-24-5 3-methoxycarbonylindole 
• 2550-36-9 Cyclohexylmethyl bromide 

Downstream Products

• 858515-52-3 C₃₈H₅₁N₃O₅ 
• 858515-71-6 1-(cyclohexylmethyl)-1H-indole-3-carboxylic acid 

Relevant academic research and scientific papers

Evaluation of carboxamide-type synthetic cannabinoids on the functional activities at cannabinoid receptors and biological effects via inhalation exposure test

Purpose: Three synthetic carboxamide-type cannabinoids (5F-MDMB-PICA, 5F-EMB-PINACA, and AMB-CHMICA) were evaluated in terms of their in vitro activities at the cannabinoid receptors CB1 and CB2 and in vivo biological effects when smoking the synthetic cannabinoids to assess their biological effects. Methods: [35S]Guanosine-5′-O-(3-thio)-triphosphate binding assays were performed to investigate the half maximal effective concentration values of the test compounds at the CB1 and CB2 receptors. Additionally, the biological effects were evaluated by observing and scoring the behavior of mice with equipment in which they inhaled smoke from a herbal mixture containing the test compounds. Results: All three synthetic cannabinoids tested in this study activated the CB1 and CB2 receptors in vitro. 5F-MDMB-PICA showed less than 1?nM of the half maximal effective concentration value for both receptors. Therefore, it was suggested that 5F-MDMB-PICA was the strongest CB1 and CB2 receptor agonist in comparison with synthetic cannabinoids evaluated in the past. The degree of the various biological effects, specifically passivity, spontaneous activity, abnormal gait, abnormal position, and grip strength, when smoking the synthetic cannabinoids corresponded to the functional activity at the CB1 receptor. However, some biological effects differed between 5F-MDMB-PICA and 5F-MDMB-PINACA, used as a positive control, and AMB-CHMICA induced some biological effects in contrast to the other tested synthetic cannabinoids. Conclusion: This study provides information regarding the biological effects when smoking synthetic cannabinoids from the functional activities at the CB1 and CB2 receptors, considering their way of inhalation and thermal degradation.

Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase

A new series of novel mast cell tryptase inhibitors is reported, which features the use of an indole structure as the hydrophobic substituent on a m-benzylaminepiperidine template. The best members of this series display good in vitro activity and excellent selectivity against other serine proteases.