Tadalafil

Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5; IC₅₀ = 1.2 nM).¹ It is selective for PDE5 over PDE1-4 and 7-10 (IC₅₀s = 9.2-280 μM), however, it does also inhibit PDE11 (IC₅₀ = 11 nM). In vivo, tadalafil (10 mg/kg) decreases production of the proinflammatory cytokines TNF-α, IL-1β, and IL-6 and improves renal function in a rat model of ischemia/reperfusion injury.² It also reduces development of tobacco smoke-induced emphysema and pulmonary hypertension in mice.³ Formulations containing tadalafil have been used to treat erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.

WARNING This product is not for human or veterinary use.

1. Card, G.L., England, B.P., Suzuki, Y., et al. Structural basis for the activity of drugs that inhibit phosphodiesterases. Structure 12(12), 2233-2247 (2004).

2. Medeiros, V.F., Azevedo, Í.M., Carvalho, M.D., et al. The renoprotective effect of oral tadalafil pretreatment on ischemia/reperfusion injury in rats. Acta Cir. Bras. 32(2), 90-97 (2017).

3. Seimetz, M., Parajuli, N., Pichl, A., et al. Cigarette smoke-induced emphysema and pulmonary hypertension can be prevented by phosphodiesterase 4 and 5 inhibition in mice. PLoS One 10(6), e0129327 (2015).

Santillo, M.F., and Mapa, M.S.T. Phosphodiesterase (PDE5) inhibition assay for rapid detection of erectile dysfunction drugs and analogs in sexual enhancement products. Drug Test Anal. 10(8), 1315-1322 (2018).