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  • Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.

Exploring the size of the lipophilic unit of the soluble epoxide hydrolase inhibitors.

Bioorganic & medicinal chemistry (2019-09-07)
Sandra Codony, Elena Valverde, Rosana Leiva, José Brea, M Isabel Loza, Christophe Morisseau, Bruce D Hammock, Santiago Vázquez
ABSTRACT

Soluble epoxide hydrolase (sEH) inhibitors are potential drugs for several diseases. Adamantyl ureas are excellent sEH inhibitors but have limited metabolic stability. Herein, we report the effect of replacing the adamantane group by alternative polycyclic hydrocarbons on sEH inhibition, solubility, permeability and metabolic stability. Compounds bearing smaller or larger polycyclic hydrocarbons than adamantane yielded all good inhibition potency of the human sEH (0.4 ≤ IC50 ≤ 21.7 nM), indicating that sEH is able to accommodate inhibitors of very different size. Human liver microsomal stability of diamantane containing inhibitors is lower than that of their corresponding adamantane counterparts.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
1-Adamantylamine, 97%
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100 μL
1 Available to ship on December 26, 2024
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0.2 mL
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Sigma-Aldrich
Anti-KDR/Flk-1/VEGFR2 Antibody, clone CH-11, clone CH-11, Upstate®, from mouse
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SKUPack SizeAvailabilityPriceQuantity
100 μL
1 Available to ship on December 26, 2024
Details...
A recombinant, preservative-free antibody is available for your target. Try ZMS1086
$523.00
0.2 mL
1 Available to ship on December 26, 2024
Details...
A recombinant, preservative-free antibody is available for your target. Try ZMS1086
$676.00