Cayman RS 17053 (hydrochloride)

RS 17053 is an α_1A-adrenergic receptor (α_1A-AR) antagonist. It selectively binds to the α_1A-AR (K_i = 2.5 nM) over α_1B- and α_1D-ARs (K_is = 50 and 79 nM, respectively). RS 17053 inhibits norepinephrine-induced contractions in isolated rat kidney and mesenteric arteries (PA₂s = 9.8 and 9.9, respectively), tissues that endogenously express high levels of α_1A-AR, and, to a lesser extent, in isolated rat aortic rings, which highly express α_1D-ARs, and human lower urinary tract tissue (PA₂s = 7.7 and 7.3, respectively). It also inhibits phenylephrine-induced increases in mean arterial pressure (MAP) in normotensive and spontaneously hypertensive rats (ED₅₀s = 528 and 533 µg/kg, respectively).

WARNING This product is not for human or veterinary use.