923565-21-3

Basic information

• Product Name: GSK962040
• Synonyms: Camicil;Camicinal;GSK962040;Lopixibat chloride;GSK962040 (Camicinal;1-[4-[(3-Fluorophenyl)amino]-1-piperidinyl]-2-[4-[[(3S)-3-methyl-1-piperazinyl]methyl]phenyl]ethanone;Ethanone, 1-[4-[(3-fluorophenyl)amino]-1-piperidinyl]-2-[4-[[(3S)-3-methyl-1-piperazinyl]methyl]phenyl]-
• CAS NO: 923565-21-3
• Molecular Formula: C25H33FN4O
• Molecular Weight: 424.55
• Mol File: 923565-21-3.mol
• Article Data: 2

Chemical Properties

• Melting Point: 144℃
• Boiling Point: 610.0±55.0 °C(Predicted)
• Appearance: /
• Density: 1.175±0.06 g/cm3(Predicted)
• PKA: 9.21±0.40(Predicted)
• CAS DataBase Reference: GSK962040(CAS DataBase Reference)
• NIST Chemistry Reference: GSK962040(923565-21-3)
• EPA Substance Registry System: GSK962040(923565-21-3)

Safety Data

• Hazardous Substances Data: 923565-21-3(Hazardous Substances Data)

Usage

General Description

GSK962040 is a selective and potent agonist of the G-protein coupled receptor GPR119, which is involved in regulating glucose homeostasis and lipid metabolism. It has been studied for its potential as a treatment for type 2 diabetes and obesity, as it has been shown to stimulate the release of incretin hormones and promote glucose-dependent insulin secretion. Additionally, GSK962040 has been found to have beneficial effects on lipid metabolism, including increasing the release of peptide YY and reducing food intake. Overall, GSK962040 has demonstrated promising potential as a therapeutic agent for conditions related to metabolic syndrome, and further research is ongoing to explore its clinical applications.

Upstream product

• 923565-93-9 phenylmethyl (2S)-4-((4-(2-(4-((3-fluorophenyl)amino)-1-piperidinyl)-2-oxoethyl)phenyl)methyl)-2-methyl-1-piperazinecarboxylate 
• 923565-74-6 1,1-dimethylethyl (2S)-4-([4-(2-(4-[(3-fluorophenyl)amino]-1-piperidinyl)-2-oxoethyl)phenyl]methyl)-2-methyl-1-piperazinecarboxylate 
• 923565-78-0 phenylmethyl (2R)-4-([4-(2-(4-[(3-fluorophenyl)amino]-1-piperidinyl)-2-oxoethyl)phenyl]methyl)-2-methyl-1-piperazinecarboxylate 

Relevant articles and documents

Discovery of N-(3-fluorophenyl)-1-[(4-([(35)-3-methyl-1-piperazinyl]methyl) phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate

N-(3-Fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl) acetyl]-4-piperidinamine 12 (GSK962040) is a novel small molecule motilin receptor agonist. It possesses excellent activity at the recombinant human motilin receptor and also at the native rabbit motilin receptor where its agonist activity results in potentiation of the amplitude of neuronal-mediated contractions of isolated gastric antrum tissue. Compound 12 also possesses highly promising pharmacokinetic profiles in both rat and dog, and these results, in combination with further profiling in human native tissue and an in vivo model of gastrointestinal transit in the rabbit, have led to its selection as a candidate for further development.