aladdin 阿拉丁 N409056 盐酸萘哌地尔 57149-08-3 10mM in DMSO

中文名：盐酸萘哌地尔

英文名：Naftopidil DiHCl

英文别名：KT-611;1-(4-(2-methoxyphenyl)piperazin-1-yl)-3-(naphthalen-1-yloxy)propan-2-ol dihydrochloride

纯度：10mM in DMSO

货号：N409056

包装：1ml

Cas号：57149-08-3

存储温度：-80℃储存

产品介绍：

Information

Naftopidil DiHCl (KT-611) is a selective5-HT1Aandα1-adrenergic receptorantagonist withIC50of 0.1 μM and 0.2 μM, respectively.
In vitro

Naftopidil diHCl possesses 5-HT1A agonistic properties in addition to being an α1-adrenoceptor antagonist. Naftopidil has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil inhibits the growth of androgen-sensitive LNCaP cells and androgen-insensitive PC-3 cells with IC50 of 22.2 μM and 33.2 μM, respectively. Cell growth inhibition by Naftopidil is due to the arrest of the G1 cell cycle. Expressions of p27^kip1 and p21^cip1 are significantly increased in LNCaP cells treated with Naftopidil. In PC-3 cells, Naftopidil induces p21^cip1 but not p27^kip1. Naftopidil produces a concentration-dependent inhibition of collagen-induced Ca²⁺ mobilization, maximum inhibition (22.9%) occurring with 40 μM Naftopidil. The adrenaline-induced rise in [Ca²⁺]_i is inhibited dose dependently by Naftopidil. Naftopidil is significantly more effective than tamsulosin in relieving nocturia. Naftopidil induces G(1) cell-cycle arrest in both PCa cells and PrSC. In Naftopidil-treated PrSC, total interleukin-6 protein is significantly reduced with increased suppression of cell proliferation.

In vivo

Oral administration of Naftopidil to nude mice inhibits the growth of PC-3 tumors as compared to vehicle-treated controls. Naftopidil improves bladder capacity and relaxed voiding via inhibition of afferent nerve activity. Naftopidil (0.1 μg–30 μg) transiently abolishes isovolumetric rhythmic bladder contraction. The amplitude of bladder contraction is decreased by intrathecal injection of naftopidil (3 μg–30 μg). Naftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model.
Cell Data

cell lines：BT474, HT1376, UMUC-3, T24, ACHN, DU-145, PC-3, LN-REC4, and LNCaP cells

Concentrations：20 μM, 40 μM

Incubation Time：24 hours

Powder Purity:≥99%

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