Silodosin - CAS:160970-54-7

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Silodosin (Synonyms:西洛多辛; KAD 3213; KMD 3213)

目录号 : KM5750 CAS No. : 160970-54-7 纯度 : 98%

Data Sheet 产品使用指南

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。

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10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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 (K_i=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with K_i 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.

体外研究

Silodosin (KAD 3213; KMD 3213) inhibits norepinephrine-induced increases in intracellular Ca 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).

RT-PCR

Cell Line:	TCCSUP; UMUC3 and 647V cells
Concentration:	0.1, 0.5, 3.0, or 10 µM
Incubation Time:	24 hours
Result:	Decreases ELK1 in bladder cancer cells.

Western Blot Analysis

Cell Line:	TCCSUP; UMUC3 and 647V cells
Concentration:	0.1, 0.5, 3.0, or 10 µM
Incubation Time:	24 hours
Result:	Decreases ELK1 in bladder cancer cells.

Cell Proliferation Assay

Cell Line:	UMUC3,TCCSUP or AR-negative 647V cells
Concentration:	0.1, 0.5, 3.0, or 10 µM
Incubation Time:	96 hours
Result:	Decreased cell viability of UMUC3 cells cultured with normal FBS containing androgens (58% decrease).

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.

分子式

C₂₅H₃₂F₃N₃O₄

分子量

495.53

CAS号

160970-54-7

中文名称

西洛多辛；西罗多辛

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (100.90 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0180 mL	10.0902 mL	20.1804 mL
5 mM	0.4036 mL	2.0180 mL	4.0361 mL
10 mM	0.2018 mL	1.0090 mL	2.0180 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.05 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.05 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.05 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。