Naftopidil (hydrochloride)

Naftopidil is an alpha1-adrenergic receptor antagonist that competitively inhibits alpha-adrenoceptor-mediated contractions induced by noradrenaline with pA2 values of 6.73-8.15 in various blood vessels from dog, rabbit, guinea pig, and rat. It binds to the cloned human alpha1-adrenergic receptors with Ki values of 3.7, 20, and 1.2 nM for alpha1A, alpha1B and alpha1D, respectively. Clinical formulations of naftopidil are used in the treatment of benign prostatic hyperplasia in Japan. Naftopidil also exhibits antiproliferative activity, inhibiting the growth of androgen-sensitive LNcaP cells and androgen-insensitive PC-3 cancer cell lines with IC50 values of 22.2 and 33.2 µM, respectively.Formal Name: 4-(2-methoxyphenyl)-alpha-[(1-naphthalenyloxy)methyl]-1-piperazineethanol, monohydrochloride. CAS Number: 1164469-60-6. Molecular Formula: C24H28N2O3 . HCl. Formula Weight: 429.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/mL, DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL, DMSO: 3 mg/mL. lambdamax: 211, 231, 288 nm. SMILES: COC1=C(N2CCN(CC(COC3=CC=CC4=C3C=CC=C4)O)CC2)C=CC=C1.Cl. InChi Code: InChI=1S/C24H28N2O3.ClH/c1-28-24-11-5-4-10-22(24)26-15-13-25(14-16-26)17-20(27)18-29-23-12-6-8-19-7-2-3-9-21(19)23,/h2-12,20,27H,13-18H2,1H3,1H. InChi Key: VQAAEWMEVIOHTJ-UHFFFAOYSA-N.