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Silodosin

CAS No. : 160970-54-7

MCE 国际站：Silodosin

产品活性：Silodosin (KAD 3213; KMD 3213) 是一个强效的、有选择性的、口服活性的 α1A-adrenergic receptor (α1A-AR) 阻滞剂。Silodosin 对 α1A-AR 表现出高度的亲和力 (K_i=0.036 nM)，是 α1B-AR 和 α1D-AR 亲和力的 162 和 50 倍，K_i 值分别为 21 nM 和 2.0 nM。Silodosin 是一种有效且耐受性良好的试剂，可用于 LUTS/BPH 的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Anti-infection

作用靶点：Adrenergic Receptor  |  Bacterial

In Vitro: Silodosin (KAD 3213; KMD 3213) inhibits norepinephrine-induced increases in intracellular Ca²⁺ concentrations in alpha 1a-AR-expressing Chinese hamster ovary cells with an IC₅₀ of 0.32 nM but had a much weaker inhibitory effect on the alpha 1b- and alpha 1d-ARs.
Silodosin potently inhibits 2-[2-(4-hydroxy-3-[125I]iodophenyl)ethylaminomethyl]-alpha-tetralone binding to the cloned human alpha 1a-AR, with a K_i value of 0.036 nM, but has 583- and 56-fold lower potency at the alpha 1b- and alpha 1d-ARs, respectively.
Silodosin (0-10 µM; 24 hours) decreases ELK1 gene expression as a dose-dependent manner in all the bladder cancer cell lines.
Silodosin (0-10 µM; 24 hours) decreases ELK1 protein expression as a as a dose-dependent manner.
Silodosin (0-10 µM; 96 hours) insignificantly changes cell viability of AR-positive UMUC3 or TCCSUP cultured in an androgen-depleted condition or that of AR-negative 647V. In contrast, silodosin reduced the growth of UMUC3 cells cultured with normal FBS containing androgens (58% decrease at 10 µM).

In Vivo: Silodosin (intravenous injection; 0.1-0.3mg/kg) reduces the obstruction-induced increases in MinP by 27.7 % (0.1 mg/kg) and 20.8 %(0.3 mg/kg). It improves detrusor overactivity and reduces the grade of obstruction, and thus may be effective for both storage and voiding dysfunction for the treatment of LUTS/BPH.

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