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Silodosin

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Chemical Structure| 160970-54-7 同义名 : KMD 3213;KAD 3213;Silodosin. trade names Rapaflo, Silodyx, Rapilif, Silodal, Urief, Urorec.
CAS号 : 160970-54-7
货号 : A632990
分子式 : C25H32F3N3O4
纯度 : 98%
分子量 : 495.534
MDL号 : MFCD00930170
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • α-adrenergic receptor
描述 Silodosin is a novel, more selective alpha-blocker, which is specific to the lower urinary tract and may have fewer side effects than other alpha-blockers[3]. Silodosin potently inhibits 2-[2-(4-hydroxy-3-[125I]iodophenyl)ethylaminomethyl]-alpha-tetralone binding to the cloned human alpha 1a-AR, with a Ki value of 0.036 nM, but has 583- and 56-fold lower potency at the alpha 1b- and alpha 1d-ARs, respectively[4]. Silodosin determines smooth muscle relaxation in bladder and prostate tissues, increases bladder blood flow in conditions of chronic bladder ischemia and regulates the activity of transcriptional factors responsible for stromal growth and prostate hyperplasia. Silodosin is one of the drugs approved for the treatment of BPH (benign prostatic hyperplasia), being highly effective in improving not only LUTS (lower urinary tract symptoms) but also urodynamic parameter impairments secondary to BPH[5]. In bladder cancer cell lines, silodosin reduced the expression of ELK1 (mRNA/protein) and its downstream target, c-fos gene, as well as the transcriptional activity of ELK1. Silodosin also inhibited the migration of ELK1-positive cells with or without a functional AR, but not that of ELK1 knockdown cells. Combined treatment with silodosin is useful for overcoming chemoresistance in patients with ELK1-positive urothelial carcinoma receiving cisplatin[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.09mL

2.02mL

1.01mL

20.18mL

4.04mL

2.02mL
参考文献

[1]Buono R, Briganti A, et al. Silodosin and tadalafil have synergistic inhibitory effects on nerve-mediated contractions of human and rat isolated prostates. Eur J Pharmacol. 2014 Dec 5;744:42-51.

[2]Tatemichi S, Kobayashi K, et al. [Alpha1-adrenoceptor subtype selectivity and organ specificity of silodosin (KMD-3213)] . Yakugaku Zasshi. 2006 Mar;126 Spec no.:209-16. Japanese.

[3]Jung JH, Kim J, MacDonald R, Reddy B, Kim MH, Dahm P. Silodosin for the treatment of lower urinary tract symptoms in men with benign prostatic hyperplasia. Cochrane Database Syst Rev. 2017;11(11):CD012615.

[4]Villa L, Buono R, Fossati N, et al. Effects by silodosin on the partially obstructed rat ureter in vivo and on human and rat isolated ureters. Br J Pharmacol. 2013;169(1):230-238

[5]Villa L, Capogrosso P, Capitanio U, et al. Silodosin: An Update on Efficacy, Safety and Clinical Indications in Urology. Adv Ther. 2019;36(1):1-18

[6]Kawahara T, Ide H, Kashiwagi E, et al. Silodosin inhibits the growth of bladder cancer cells and enhances the cytotoxic activity of cisplatin via ELK1 inactivation. Am J Cancer Res. 2015;5(10):2959-2968.