製品番号: HY-B0661

Tamsulosin

(別名: (R)-(-)-YM12617 free base; LY253351 free base)

2 Cited Publications

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Tamsulosin ((R)-(-)-YM12617 free base) is an orally active antagonist of α₁-adrenergic receptor. Tamsulosin induces Apoptosis. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models.

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純度: 99.80%
CAS 番号: 106133-20-4
分子式: C₂₀H₂₈N₂O₅S
分子量:408.51

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Tamsulosin 構造式

CAS 番号: 106133-20-4

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数量

Amount: USD 0.00

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (2)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

α1-adrenergic receptor

Adrenergic Receptor アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	EC₅₀	0.13 nM Compound: Tamsulosin	Intrinsic activity at human alpha1B adrenergic receptor expressed in CHOK1 cells co-expressing aequorin assessed as inhibition of agonist induced calcium mobilization preincubated for 15 mins followed by agonist addition measured for 20 secs in presence o Intrinsic activity at human alpha1B adrenergic receptor expressed in CHOK1 cells co-expressing aequorin assessed as inhibition of agonist induced calcium mobilization preincubated for 15 mins followed by agonist addition measured for 20 secs in presence o	[PMID: 27658792]
HEK293	IC₅₀	1.4 nM Compound: 1	Antagonist activity at human full-length N-terminal SNAP-tagged alpha1D adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assa Antagonist activity at human full-length N-terminal SNAP-tagged alpha1D adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assa	[PMID: 27709945]
HEK293	IC₅₀	2.2 nM Compound: 1	Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assa Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assa	[PMID: 27709945]
HEK293	IC₅₀	4.8 nM Compound: 1	Antagonist activity at human full-length N-terminal SNAP-tagged alpha1B adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assa Antagonist activity at human full-length N-terminal SNAP-tagged alpha1B adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assa	[PMID: 27709945]

体外実験

Tamsulosin shows intrinsic activity at human alpha1B adrenergic receptor expressed in CHOK1 cells co-expressing aequorin, with EC₅₀ of 0.13 nM^[2].
Tamsulosin (25-50 nM, 24 h) attenuates high glucose-induced injury in glomerular endothelial cells^[3].
Tamsulosin (1-100 μM, 5 days) significantly influences ECM production and distribution as well as cellular metabolism levels in ARPE 19 cells in a concentration-dependent manner^[4].
. Tamsulosin (50-400 μM, 24 h) induces apoptosis and clusterin expression in NRP-152 cells^[5].
.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR^[3]

Cell Line:

Human glomerular endothelial cells (GECs)
Concentration:

25, and 50 nM
Incubation Time:

24 h
Result:

Attenuated high glucose-induced expression of pro-inflammatory cytokines IL-6, TNF-α, and IL-8.
Reduced MMP-2 and MMP-9.
Prevented high glucose-induced expression of VCAM-1 and ICAM-1.
Decreased Col-1 and TGF-β1.

Western Blot Analysis^[3]

Cell Line:

Human glomerular endothelial cells (GECs)
Concentration:

25, and 50 nM
Incubation Time:

24 h
Result:

Decreased nuclear NF-κB p65 to 2.7- and 1.9- fold at 25 and 50 nM, respectively.

体内実験

Tamsulosin (0.001-1 mg/kg, gavage, subacutely, 3 doses within 24 h (1, 5 and 23 h) or acutely 60 min before the behavioral tests) facilitates depressive-like behaviors through endogenous glucocorticoids in mice^[6].
Tamsulosin (0.01-1 mg/kg, p.o., once a day for 14 consecutive days) exerts inhibitory effect on neuronal activation in the voiding centers of rats with Cyclophosphamide (HY-17420)-induced overactive bladder^[7].
Tamsulosin (17.5-35 mcg/kg/d, p.o.) results in protection from respiratory inflammatory events in rats with induced airway sensitization^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

化学情報

CAS 番号 106133-20-4
性状 Solid
分子量 408.51
分子式 C₂₀H₂₈N₂O₅S
Color White to off-white
SMILES

O=S(C1=CC(C[C@H](NCCOC2=CC=CC=C2OCC)C)=CC=C1OC)(N)=O
別名

(R)-(-)-YM12617 free base; LY253351 free base
Structure Classification
- Alkaloids
- Other Alkaloids
Initial Source
- Endogenous metabolite
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Journal Impact Factor

Nat Commun

A gatekeeper sympathetic control of lacrimal tear secretion and dry eye onset through the NA-Adra1a-Ucp2 pathway. [Abstract]

2025 Jun 5;16(1):5215. PMID: 40473608
Invest Ophthalmol Vis Sci

Activation of Sympathetic Nervous System Drives Dry Eye Onset Via Norepinephrine-β2-Adrenergic Receptor Signaling in Mice. [Abstract]

2025 Jun 2;66(6):13. PMID: 40465266

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (244.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4479 mL

12.2396 mL

24.4792 mL

5 mM

0.4896 mL

2.4479 mL

4.8958 mL

10 mM

0.2448 mL

1.2240 mL

2.4479 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
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OR (2659 KB)
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取扱説明書 (2659 KB)

参考文献

[1]. Christopher Chapple, et al. Tamsulosin: an overview. World J Urol. 2002 Apr;19(6):397-404. [Content Brief]

[2]. Rak A, et al. Arylsulfonamide derivatives of (aryloxy)ethyl pyrrolidines and piperidines as α1-adrenergic receptor antagonist with uro-selective activity. Bioorg Med Chem. 2016 Nov 1;24(21):5582-5591. [Content Brief]

[3]. Sun L, et al. Tamsulosin attenuates high glucose- induced injury in glomerular endothelial cells. Bioengineered. 2021 Dec;12(1):5184-5194. [Content Brief]

[4]. Ida Y, et al. The Selective α1 Antagonist Tamsulosin Alters ECM Distributions and Cellular Metabolic Functions of ARPE 19 Cells in a Concentration-Dependent Manner. Bioengineering (Basel). 2022 Oct 14;9(10):556. [Content Brief]

[5]. Youm Y H, et al. Apoptosis Induction and Clusterin Expression of NRP-152 Cells by Tamsulosin. Journal of the Korean Continence Society, 2006, 10(2): 132-139.

[6]. Holanda VAD, et al. Tamsulosin facilitates depressive-like behaviors in mice: Involvement of endogenous glucocorticoids. Brain Res Bull. 2022 Jan;178:29-36. [Content Brief]

[7]. Kim SE, et al. Effects of Tamsulosin on Urinary Bladder Function and Neuronal Activity in the Voiding Centers of Rats with Cyclophosphamide-induced Overactive Bladder. Int Neurourol J. 2012 Mar;16(1):13-22. [Content Brief]

[8]. Alabdali H H, et al. Study the anti-inflammatory effects of tamsulosin by the evaluation of inflammatory cells and lung histopathology in an airway inflammation model in rats. Bulletin of Pharmaceutical Sciences. Assiut, 2023, 46(1): 633-645.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4479 mL	12.2396 mL	24.4792 mL	61.1980 mL
	5 mM	0.4896 mL	2.4479 mL	4.8958 mL	12.2396 mL
	10 mM	0.2448 mL	1.2240 mL	2.4479 mL	6.1198 mL
	15 mM	0.1632 mL	0.8160 mL	1.6319 mL	4.0799 mL
	20 mM	0.1224 mL	0.6120 mL	1.2240 mL	3.0599 mL
	25 mM	0.0979 mL	0.4896 mL	0.9792 mL	2.4479 mL
	30 mM	0.0816 mL	0.4080 mL	0.8160 mL	2.0399 mL
	40 mM	0.0612 mL	0.3060 mL	0.6120 mL	1.5300 mL
	50 mM	0.0490 mL	0.2448 mL	0.4896 mL	1.2240 mL
	60 mM	0.0408 mL	0.2040 mL	0.4080 mL	1.0200 mL
	80 mM	0.0306 mL	0.1530 mL	0.3060 mL	0.7650 mL
	100 mM	0.0245 mL	0.1224 mL	0.2448 mL	0.6120 mL

Keywords

Tamsulosin

2 Cited Publications

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Tamsulosin

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MedChemExpress（MCE）の使用を引用している文献 Tamsulosin

Adrenergic Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Tamsulosin 関連分類

製品番号: HY-B0661