Description
Candesartan is an inhibitor of the angiotensin II type 1 receptor (AT1) that displays antihypertensive, cardioprotective, nephroprotective, and potentially antiviral activities. In vivo, candesartan increases renal blood blow and decreases renal vascular resistance, glomerular filtration rate, and filtration fraction. Candesartan also decreases NADPH oxidase activity and levels of TGF-β, inhibiting calcium oxalate crystal deposition and kidney stone formation. In animal models of pressure overload-induced cardiac remodeling, candesartan downregulates Smad3 and fibronectin, upregulates Smad7, and inhibits matrix metalloproteinase 9 (MMP9) and the epithelial-to-mesenchymal transition (EMT), preventing collagen deposition, left ventricular remodeling, and decreases in left ventricular ejection fraction. Additionally, this compound downregulates expression of VEGFR2, decreasing retinal neovascularization without inhibiting total angiogenesis. Separately, candesartan may inhibit the interaction between lens epithelium-derived growth factor (LEDGF) and HIV-1 integrase, exhibiting potential as a treatment for HIV.
References
Patinha D, Fasching A, Pinho D, et al. Angiotensin II contributes to glomerular hyperfiltration in diabetic rats independently of adenosine type I receptors. Am J Physiol Renal Physiol. 2013 Mar 1;304(5):F614-22. PMID: 23283998.
Hu G, Li X, Sun X, et al. Identification of old drugs as potential inhibitors of HIV-1 integrase - human LEDGF/p75 interaction via molecular docking. J Mol Model. 2012 Dec;18(12):4995-5003. PMID: 22733274.
Nakamura S, Tsuruma K, Shimazawa M, et al. Candesartan, an angiotensin II type 1 receptor antagonist, inhibits pathological retinal neovascularization by downregulating VEGF receptor-2 expression. Eur J Pharmacol. 2012 Jun 15;685(1-3):8-14. PMID: 22543084.
Yu H, Zhao G, Li H, et al. Candesartan antagonizes pressure overload-evoked cardiac remodeling through Smad7 gene-dependent MMP-9 suppression. Gene. 2012 Apr 15;497(2):301-6. PMID: 22326534.
Yoshioka I, Tsujihata M, Akanae W, et al. Angiotensin type-1 receptor blocker candesartan inhibits calcium oxalate crystal deposition in ethylene glycol-treated rat kidneys. Urology. 2011 Apr;77(4):1007.e9-1007.e14. PMID: 21256551.
Wada T, Inada Y, Ojima M, et al. Comparison of the antihypertensive effects of the new angiotensin II (AT1) receptor antagonist candesartan cilexetil (TCV-116) and the angiotensin converting enzyme inhibitor enalapril in rats. Hypertens Res. 1996 Jun;19(2):75-81. Erratum in: Hypertens Res 1996 Sep;19(3):221. PMID: 10968199.
ABOUT LKT LABS
LKT Laboratories is a biochemical supply company focused on the synthesis, purification, and isolation of small molecules for research applications. Its range of products exhibit known biological activities that have found uses in a wide array of research fields, especially cancer and neuroscience. These products include protein kinase inhibitors, ion channel modulators, and activators. LKT serves the global research community by supplying the highest purity products for use in cell culture models, animal studies, or as reference materials or analytical standards.
