Valsartan (137862-53-4) is a high affinity angiotensin AT1 receptor antagonist (Ki = 2.38 nM). Highly selective (30,000-fold) over AT2 receptors1,2. Normalizes the increased production of inflammatory cytokines in adipose and liver tissue in LPS-infused mice3. Valsartan is a clinically useful antihypertensive agent. Orally active.
1) Criscione et al. (1993), Pharmacological profile of valsartan: a potent, orally active, nonpeptide antagonist of the angiotensin II AT1-receptor subtype; Br. J. Pharmacol., 110 761
2) Wexler et al. (1996), Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy; J. Med. Chem., 39 625
3) Iwashita et al. (2013), Valsartan restores inflammatory response by macrophages in adipose and hepatic tissues of LPS-infused mice; Adipocyte, 2 28