RS 17053 (hydrochloride)

RS 17053 is an alpha1A-adrenergic receptor (alpha1A-AR) antagonist. It selectively binds to the alpha1A-AR (Ki = 2.5 nM) over alpha1B- and alpha1D-ARs (Kis = 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 alpha1A-AR, and, to a lesser extent, in isolated rat aortic rings, which highly express alpha1D-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).Formal Name: 5-chloro-N-[2-[2-(cyclopropylmethoxy)phenoxy]ethyl]-alpha,alpha-dimethyl-1H-indole-3-ethanamine, monohydrochloride. CAS Number: 169505-93-5. Molecular Formula: C24H29ClN2O2 . HCl. Formula Weight: 449.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 50 mM, Ethanol: 10 mM. SMILES: CC(NCCOC1=C(OCC2CC2)C=CC=C1)(C)CC3=CNC4=C3C=C(Cl)C=C4.Cl. InChi Code: InChI=1S/C24H29ClN2O2.ClH/c1-24(2,14-18-15-26-21-10-9-19(25)13-20(18)21)27-11-12-28-22-5-3-4-6-23(22)29-16-17-7-8-17,/h3-6,9-10,13,15,17,26-27H,7-8,11-12,14,16H2,1-2H3,1H. InChi Key: QFOPFGRPNPCPBX-UHFFFAOYSA-N.