产品
编 号：F192885
分子式：C25H32F3N3O4
分子量：495.53
分子式：C25H32F3N3O4
分子量：495.53
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
320
In-stock
10mg
520
In-stock
50mg
1984
In-stock
100mg
3080
In-stock
结构图
CAS No: 160970-54-7
产品详情
生物活性：
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.
体内研究：
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.Animal Model:Sprague Dawley rats
Dosage:0.1-0.3mg/kg
Administration:Intravenous injection
Result:Effectively reduced contractions of both human and rat isolated ureters.
体外研究：
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 Ki 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 UMUC3or 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).
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.
体内研究：
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.Animal Model:Sprague Dawley rats
Dosage:0.1-0.3mg/kg
Administration:Intravenous injection
Result:Effectively reduced contractions of both human and rat isolated ureters.
体外研究：
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 Ki 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 UMUC3or 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).
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