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MK 0686

CAT: 0804-HY-15042-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-15042-01Size:5 mg
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Description
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[1].
CAS Number
[578727-68-1]
UNSPSC
12352005
Target
Bradykinin Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Metabolic Disease
Assay Protocol
https://www.medchemexpress.com/mk-0686.html
Purity
99.76
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(C(F)(F)F)NC1(C(N[C@H](C)C2=C(F)C=C(C3=CC=CC(Cl)=C3C(OC)=O)C=C2)=O)CC1
Molecular Formula
C22H19ClF4N2O4
Molecular Weight
486.84
References & Citations
[1]CYP2C75-Involved Autoinduction of Metabolism in Rhesus Monkeys of Methyl 3-Chloro-3′-fluoro-4′-{ (1R) -1-[ ({1-[ (trifluoroacetyl) amino]cyclopropyl}carbonyl) amino]ethyl}-1,1′-biphenyl-2-carboxylate (MK-0686), a Bradykinin B1 Receptor Antagonist
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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