Naftopidil (hydrochloride) (KT-611 hydrochloride) 是一种选择性 alpha1-adrenoceptor 拮抗剂，对克隆的人 α1a-、α1b- 和 α1d-adrenoceptor 亚型的 Kis 分别为 3.7 nM、20 nM 和 1.2 nM。 Naftopidil（盐酸盐）具有抗增殖作用。 Naftopidil（盐酸盐）可用于前列腺增生的研究。
| Cas No. | 1164469-60-6 |
| 别名 | KT-611 hydrochloride; BM-15275 hydrochloride |
| Canonical SMILES | COC1=C(N2CCN(CC(COC3=CC=CC4=C3C=CC=C4)O)CC2)C=CC=C1.Cl |
| 分子式 | C24H28N2O3•HCl |
| 分子量 | 429 |
| 溶解度 | DMF: 10 mg/mL,DMF:PBS (pH 7.2) (1:4): 0.2 mg/mL,DMSO: 3 mg/mL |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Naftopidil is an α1-adrenergic receptor antagonist that competitively inhibits α-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 α1-adrenergic receptors with Ki values of 3.7, 20, and 1.2 nM for α1A, α1B and α1D, 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. |
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