Angiotensin AT1 receptor antagonist. Hypertension drug in clinical trials to treat COVID-19.
- Datasheet: view or download
- Applications:Approved drug (U.S.); in COVID-19 clinical trials
Biochemicals & reagents
1) Criscione et al. (1993), Pharmacological profile of calsartan: 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
Valsartan is a high affinity angiotensin AT1 receptor antagonist (Ki = 2.38 nM) and is highly selective (30,000-fold) over AT2 receptors (1,2). This compound normalizes the increased production of inflammatory cytokines in adipose and liver tissue in LPS-infused mice (3) and is also a clinically relevant antihypertensive agent being orally active.