1030612-87-3

Basic information

• Product Name: MK-8245
• Synonyms: MK-8245;2-(5-(5-(4-(2-bromo-5-fluorophenoxy)piperidin-1-yl)-1,3,4-thiadiazol-2-yl)-2H-tetrazol-2-yl)acetic acid;(5-{5-[4-(2-broMo-5-fluorophenoxy)piperidin-1-yl]-[1,3,4]-thiadiazol-2-yl}-2H-tetrazol-2-yl)acetic acid;5-[5-[4-(2-Bromo-5-fluorophenoxy)-1-piperidinyl]-1,3,4-thiadiazol-2-yl]-2H-tetrazole-2-acetic acid;2-(5-(5-(4-(2-Bromo-5-fluorophenoxy)piperidin-1-yl)-1,3,4-thiadiazol-2-yl)-2H-tetrazol-2-yl)aceti;2-(5-(5-(4-(2-Bromo-5-fluorophenoxy)piperidin-1-yl)-1,3,4-thiadiazol-2-yl)-2H-tetrazol-2-yl)ac
• CAS NO: 1030612-87-3
• Molecular Formula: C₁₆H₁₅BrFN₇O₃S
• Molecular Weight: 484.3028032
• EINECS: -0
• Mol File: 1030612-87-3.mol
• Article Data: 1

Chemical Properties

• Appearance: /
• CAS DataBase Reference: MK-8245(CAS DataBase Reference)
• NIST Chemistry Reference: MK-8245(1030612-87-3)
• EPA Substance Registry System: MK-8245(1030612-87-3)

Safety Data

• Hazardous Substances Data: 1030612-87-3(Hazardous Substances Data)

Usage

Description

MK-8245 is a potent and selective inhibitor of liver-specific phosphodiesterase 3 (PDE3), a key enzyme involved in the regulation of hepatic glucose and lipid metabolism. Its ability to inhibit PDE3 suggests that MK-8245 could enhance insulin sensitivity and decrease liver fat content, positioning it as a promising candidate for the treatment of non-alcoholic steatohepatitis (NASH) and other metabolic disorders.
Used in Pharmaceutical Industry:
MK-8245 is used as a therapeutic agent for the treatment of non-alcoholic steatohepatitis (NASH) and other metabolic disorders due to its potential to improve insulin sensitivity and reduce liver fat content.
Used in Metabolic Disorder Management:
MK-8245 is used as a treatment to enhance insulin sensitivity and improve glucose and lipid metabolism, addressing the growing epidemic of metabolic diseases, including NASH and type 2 diabetes.
Used in Preclinical Research:
MK-8245 is used as a subject of preclinical studies to evaluate its pharmacokinetic properties and efficacy in reducing liver fat accumulation, providing insights into its potential as a novel therapeutic approach for metabolic diseases.

Upstream product

• 147460-41-1 2-bromo-5-fluorophenol 
• 109384-19-2 t-butyl 4-hydroxy piperidine-1-carboxylate 
• 1030613-22-9 ethyl (5-{5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3,4-thiadiazol-2-yl}-2H-tetrazol-2-yl)acetate 
• 1030613-20-7 4-(2-bromo-5-fluorophenoxy)-1-[5-(2H-tetrazol-5-yl)-1,3,4-thiadiazol-2-yl]piperidine 
• 1020658-57-4 5-[4-(2-bromo-5-fluorophenoxy)piperidin-1-yl]-1,3,4-thiadiazole-2-carbonitrile 
• 916971-27-2 4-(2-bromo-5-fluorophenoxy)piperidine 

Relevant articles and documents

Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia

The potential use of SCD inhibitors for the chronic treatment of diabetes and dyslipidemia has been limited by preclinical adverse events associated with inhibition of SCD in skin and eye tissues. To establish a therapeutic window, we embarked on designing liver-targeted SCD inhibitors by utilizing molecular recognition by liver-specific organic anion transporting polypeptides (OATPs). In doing so, we set out to target the SCD inhibitor to the organ believed to be responsible for the therapeutic efficacy (liver) while minimizing its exposure in the tissues associated with mechanism-based SCD depletion of essential lubricating lipids (skin and eye). These efforts led to the discovery of MK-8245 (7), a potent, liver-targeted SCD inhibitor with preclinical antidiabetic and antidyslipidemic efficacy with a significantly improved therapeutic window.