1037792-44-1

Basic information

• Product Name: MBX2982
• Synonyms: MBX2982;5-Ethyl-2-[4-[4-[[[4-(1H-tetrazol-1-yl)phenyl]oxy]methyl]thiazol-2-yl]piperidin-1-yl]pyrimidine;MBX2982 / MBX-2982;5-Ethyl-2-[4-[4-[[[4-(1H-tetrazol-1-yl)phenyl]oxy]methyl]thiazol-2-yl]piperidin-1-yl]pyrimidine MBX-2982;pyrimidine, 5-ethyl-2-[4-[4-[[4-(1h-tetrazol-1-yl)phenoxy]methyl]-2-thiazolyl]-1-piperidinyl]-;2-[1-(5-ethylpyrimidin-2-yl)-4-piperidyl]-4-[[4-(tetrazol-1-yl)phenoxy]methyl]thiazole;MBX-2982, >=98%;SAR-260093
• CAS NO: 1037792-44-1
• Molecular Formula: C₂₂H₂₄N₈OS
• Molecular Weight: 448.54396
• Product Categories: Inhibitors
• Mol File: 1037792-44-1.mol
• Article Data: 4

Chemical Properties

• Boiling Point: 683.6±65.0 °C(Predicted)
• Appearance: /
• Density: 1.42
• PKA: 5.39±0.42(Predicted)
• CAS DataBase Reference: MBX2982(CAS DataBase Reference)
• NIST Chemistry Reference: MBX2982(1037792-44-1)
• EPA Substance Registry System: MBX2982(1037792-44-1)

Safety Data

• Hazardous Substances Data: 1037792-44-1(Hazardous Substances Data)

Usage

Description

MBX-2982 is an agonist of GPR119, a G-protein coupled receptor that plays a role in glucose homeostasis and lipid metabolism. It has been shown to reduce the protein levels of sterol regulatory element binding protein 1 (SREBP-1) in HepG2 cells and rat primary hepatocytes under high-glucose and -insulin conditions. Additionally, MBX-2982 has been demonstrated to inhibit hepatic lipid accumulation in mice fed a high-fat diet and increase plasma levels of glucagon-like peptide 1 (GLP-1) and glucokinase activity.

Uses

Used in Pharmaceutical Industry:
MBX-2982 is used as a potential treatment for metabolic disorders such as diabetes and obesity. Its ability to reduce SREBP-1 levels and inhibit hepatic lipid accumulation suggests that it may have therapeutic potential in the treatment of these conditions.
Used in Research Applications:
MBX-2982 is used as a research tool to study the role of GPR119 in glucose homeostasis and lipid metabolism. It can be used to investigate the mechanisms by which GPR119 agonists may improve metabolic function and to identify potential targets for the development of new therapies for metabolic disorders.
Used in Drug Development:
MBX-2982 may be used in the development of new drugs targeting GPR119 for the treatment of metabolic disorders. Its effects on SREBP-1 levels, hepatic lipid accumulation, and GLP-1 and glucokinase activity make it a promising candidate for further research and development in this area.

Upstream product

• 1282042-63-0 4-[4-(4-tetrazol-1-yl-phenoxymethyl)thiazol-2-yl]piperidine hydrochloride 
• 111196-81-7 2-chloro-5-ethylpyrimidine 
• 64001-11-2 1-(4-hydroxyphenyl)-1H-1,2,3,4-tetrazole 
• 650579-82-1 1,1-dimethylethyl 4-[4-(chloromethyl)-1,3-thiazol-2-yl]piperidine-1-carboxylate 
• 39546-32-2 4-carboxamidopiperidine 
• 1037797-53-7 4-((4-(1H-tetrazol-1-yl)phenoxy)methyl)-2-(piperidin-4-yl)thiazole 
• 123-30-8 4-amino-phenol 
• 1037797-49-1 2-[4-(4-chloromethylthiazol-2-yl)piperidin-1-yl]-5-ethylpyrimidine 

Relevant articles and documents

Synthesis and biological evaluation of thiazole derivatives as GPR119 agonists

A series of 4-(phenoxymethyl)thiazole derivatives was synthesized and evaluated for their GPR119 agonistic effect. Several 4-(phenoxymethyl)thiazoles with pyrrolidine-2,5-dione moieties showed potent GPR119 agonistic activities. Among them, compound 27 and 32d showed good in vitro activity with an EC50 value of 49 nM and 18 nM, respectively with improved human and rat liver microsomal stability compare with MBX-2982. Compound 27 & 32d did not exhibit significant CYP inhibition, hERG binding, and cytotoxicity. Moreover, these compounds lowered the glucose excursion in mice in an oral glucose-tolerance test.

PREPARATION OF 5-ETHYL-2-{4-[4-(4-TETRAZOL-1-YL-PHENOXYMETHYL)-THIAZOL-2-YL]-PIPERIDIN-1-YL}-PYRIMIDINE

Processes and intermediates for the synthesis of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine are provided.