Irbesartan
Irbesartan is an angiotensin II type 1 (AT1) receptor inhibitor that also activates PPARγ receptors; it exhibits antihypertensive, cardioprotective, and anti-hyperlipidemic activities. In angiotensin-converting enzyme 2 (ACE2)-deficient mice, irbesartan decreases TGF-β1, atrial natriuretic factor, collagen, and phospho-ERK1/2 expression and increases PPARγ expression, reversing cardiac hypertrophy and myocardial fibrosis. In animal models of angiotensin II (ATII)-mediated abdominal aortic aneurysm, irbesartan prevents macrophage infiltration, pro-inflammatory cytokine release, smooth muscle attenuation, and medial elastolysis, and also limits aneurysm enlargement. In obese hypertensive rats, this compound decreases plasma levels of free fatty acids, triglycerides, and insulin; it also upregulates expression of hepatic PPARα. In high fat diet rats, irbesartan decreases body weight and adipose tissue weight and improves glucose metabolism and vascular function.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18931690
| Cas No. |
138402-11-6 |
|---|---|
| Purity |
≥98% |
| Formula |
C25H28N6O |
| Formula Wt. |
428.53 |
| Chemical Name |
2-Butyl-3-[[2’-(1H-tetrazol-5-yl)[1,1’-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4,4]non-1-en-4-one |
| IUPAC Name |
2-butyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one |
| Synonym |
Aprovel, Avapro |
| Melting Point |
180-181°C |
| Appearance |
White to off white powder |
Zhang ZZ, Shang QH, Jin HY, et al. Cardiac protective effects of irbesartan via the PPAR-gamma signaling pathway in angiotensin-converting enzyme 2-deficient mice. J Transl Med. 2013 Sep 25;11(1):229. PMID: 24067190.
Iida Y, Xu B, Schultz GM, et al. Efficacy and mechanism of angiotensin II receptor blocker treatment in experimental abdominal aortic aneurysms. PLoS One. 2012;7(12):e49642. PMID: 23226500
Rong X, Li Y, Ebihara K, et al. Irbesartan treatment up-regulates hepatic expression of PPARalpha and its target genes in obese Koletsky (fa(k)/fa(k)) rats: a link to amelioration of hypertriglyceridaemia. Br J Pharmacol. 2010 Aug;160(7):1796-807. PMID: 20649581
de las Heras N, Martín-Fernández B, Miana M, et al. The protective effect of irbesartan in rats fed a high fat diet is associated with modification of leptin-adiponectin imbalance. J Hypertens Suppl. 2009 Aug;27(6):S37-41. PMID: 19633450.
Siragy H. Angiotensin II receptor blockers: review of the binding characteristics. Am J Cardiol. 1999 Nov 18;84(10A):3S-8S. PMID: 10588088.
