MK 0686

Overview

MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals . The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time.

Application

Products | Products > Disease Areas > Metabolic or Endocrine Disease | Products > Signaling Pathways > GPCR/G Protein | Products > Research Areas > Metabolic Disease | Products > Signaling Pathways > Bradykinin Receptor

Product Information

• Catalog No.: HY-15042
• CAS No.: 578727-68-1
• Molecular Formula: C22H19ClF4N2O4
• Molecular Weight: 486.84
• Purity: 99.76%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution
• Availability: In-stock

Source

Original product source