603139-12-4

Basic information

• Product Name: MK-0822
• CAS NO: 603139-12-4
• Mol File: 603139-12-4.mol
• Article Data: 7

Chemical Properties

• CAS DataBase Reference: MK-0822(CAS DataBase Reference)
• NIST Chemistry Reference: MK-0822(603139-12-4)
• EPA Substance Registry System: MK-0822(603139-12-4)

Safety Data

• Hazardous Substances Data: 603139-12-4(Hazardous Substances Data)

Usage

General Description

MK-0822, also known as lorcaserin, is a chemical compound that functions as a selective serotonin 2C receptor agonist. It is used as a prescription medication for the treatment of obesity and weight management. Lorcaserin works by activating serotonin receptors in the brain, which helps to reduce appetite and promote a feeling of fullness. It is often prescribed as part of a comprehensive weight loss program that includes diet and exercise. However, due to safety concerns related to potential increased risk of cancer and heart valve issues, MK-0822 has been withdrawn from the market in several countries. Nevertheless, it remains available in some regions under strict medical supervision.

Upstream product

• 7533-40-6 (S)-2-amino-4-methylpentan-1-ol 
• 603142-80-9 (2S)-2-[(1S)-1-(4-bromo-phenyl)-2,2,2-trifluoro-ethylamino]-4-methyl-pentan-1-ol 
• 98546-51-1 (4-thiomethoxyphenyl)boronic acid 
• 603142-82-1 (2S)-4-methyl-2-[(1S)-2,2,2-trifluoro-1-(4'-methylsulfonyl-biphenyl-4-yl)ethylamino]-pentan-1-ol 
• 896743-08-1 [(1S)-1-(4-bromo-phenyl)-2,2,2-trifluoro-ethyl]-((1S)-3-methyl-1-triethylsilanyloxymethyl-butyl)-amine 
• 603142-81-0 (2S)-4-methyl-2-[(1S)-2,2,2-trifluoro-1-(4'-methylsulfanyl-biphenyl-4-yl)ethylamino]-pentan-1-ol 
• 896743-07-0 ((S)-3-methyl-1-triethylsilanyloxymethyl-butyl)-[2,2,2-trifluoro-eth-(E)-ylidene]amine 
• 896743-06-9 (S)-3-methyl-1-triethylsilanyloxymethyl-butylamine 
• 603142-83-2 (S)-4-methyl-2-(((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)ethyl)amino)pentanoic acid 
• 540-61-4 2-aminoacetonitrile 
• 934482-26-5 N-{(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl}-L-leucylglycinamide 
• 6011-14-9 2-aminoacetonitrile hydrochloride 

Relevant articles and documents

Primary amides as selective inhibitors of cathepsin K

The nitrile warhead used in a series of cathepsin K inhibitors can be replaced by a less electrophilic primary amide. The accompanying loss of potency can be partially recovered by introducing a substituent α to the amide. The potency gain resulting from this addition is not achieved with the nitrile derivatives due to a different geometry of the cysteine adduct in the enzyme active site. This study led to the identification of the primary amide 2g, which is an inhibitory substrate, with an IC50 of 10 nM against cathepsin K and excellent selectivity versus the other cathepsins.

Diastereoselective arylithium addition to an α-trifluoromethyl imine. Practical synthesis of a potent cathepsin K inhibitor

A practical, chromatography-free synthesis of potent cathepsin K inhibitor 1 is described. The addition of 4-bromophenyllithium to an α- trifluoromethylimine derived from commercially available (S)-leucinol was accomplished in a highly diastereoselective

CATHEPSIN CYSTEINE PROTEASE INHIBITORS

This invention relates to a novel class of compounds, represented by the formula below, wherein the meanings of G, E, E, n, R1, R2, R3 et R4 are indicated therein, which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.