20-HETE is an important metabolite of arachidonic acid in the vasculature, especially in the kidney, where it is synthesized by cytochrome P450 (CYP450) enzymes of the 4A family.1,2 Alkylaryl imidazoles have been previously shown to inhibit certain CYP450 enzymes, including the CYP4A enzymes associated with 20-HETE synthesis.3 CAY10434 is a selective inhibitor of the 20-HETE synthase CYP4A11 exhibiting an IC50 value of 8.8 nM when tested in human renal microsomes.4 CAY10434 is nearly 200 times less potent as an inhibitor of 1A, 1C, and 3A CYP450 enzymes.
1Harder, D.R., Lange, A.R., Gebremedhin, D., et al. Cytochrome P450 metabolites of arachidonic acid as intracellular signaling molecules in vascular tissue. J Vasc Res34237-243(1997).
2Imig, J.D., Zou, A.P., Stec, D.E., et al. Formation and actions of 20-hydroxyeicosatetraenoic acid in rat renal arterioles.. Am J Physiol270R217-R227(1996).
3Nakamura, T., Sato, M., Kakinuma, H., et al. Pyrazole and isoxazole derivatives as new, potent, and selective 20-hydroxy-5,8,11,14-eicosatetraenoic acid synthase inhibitors. J Med Chem465416-5427(2003).
4Nakamura, T., Kakinuma, H., Umemiya, H., et al. Imidazole derivatives as new potent and selective 20-HETE synthase inhibitor. Bioorg Med Chem Lett14333-336(2004).
Cayman Chemical Company regularly evaluates our shipping methods to ensure product stability is maintained and our corporate environmental impact is minimized. Products selected for review are evaluated and shipping methods are certified by our Scientists. While occasionally our method of shipping a product may change, rest assured the shipping conditions on all Cayman Chemical products have been reviewed and validated.
Upon receipt, it is important to check the storage requirements of your products and place them at the appropriate temperature. Products shipped without ice may require frozen storage for long term stability.
Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.
Manufacturer, supplier, and vendor of biochemical reagents, assay kits, forensic chemistry standards, antibodies, and proteins for scientific research
Analytical testing services and custom synthesis also available