Silodosin


CAS No. : 160970-54-7

(Synonyms: KAD 3213; KMD 3213)

160970-54-7
Price and Availability of CAS No. : 160970-54-7
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Cat. No. : HY-10122
M.Wt: 495.53
Formula: C25H32F3N3O4
Purity: >98 %
Solubility: DMSO : ≥ 50 mg/mL (100.90 mM)
Introduction of 160970-54-7 :

Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3]. IC50 & Target: Ki: 0.036 nM (α1A-AR); 21 nM (α1B-AR); 2 nM (α1D-AR)[1] 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[1].
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[2].
Silodosin (0-10 µM; 24 hours) decreases ELK1 gene expression as a dose-dependent manner in all the bladder cancer cell lines[4].
Silodosin (0-10 µM; 24 hours) decreases ELK1 protein expression as a as a dose-dependent manner[4].
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)[4].
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[2].

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