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Tamsulosin

Name: Tamsulosin
Brand: TargetMol
SKU: T0210L
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0210LCas No. 106133-20-4

Alias LY253351 free base, HSDB-7744, HSDB7744, HSDB 7744, Harnal-D, Flowmax, (R)-(-)-YM12617 free base

Tamsulosin ((R)-(-)-YM12617 free base) is an alpha1A adrenergic receptor antagonist used for the symptomatic treatment of benign prostatic hyperplasia (BPH). It treats difficulty urinating, a common symptom of an enlarged prostate, by relaxing the neck muscles of the bladder and muscle fibers in the prostate itself, easing urination.

Tamsulosin

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Purity: 99.93%

Catalog No. T0210LAlias LY253351 free base, HSDB-7744, HSDB7744, HSDB 7744, Harnal-D, Flowmax, (R)-(-)-YM12617 free baseCas No. 106133-20-4

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$30	-	In Stock
25 mg	$48	-	In Stock
50 mg	$68	-	In Stock
100 mg	$98	-	In Stock
1 mL x 10 mM (in DMSO)	$29	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.93%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Tamsulosin AI Summary

Tamsulosin is a highly potent compound with significant binding affinity across multiple adrenergic receptor subtypes. It displays exceptionally low Ki values for human Alpha-1A (0.029 nM), Alpha-1B (0.61 nM), and Alpha-1D (0.058 nM) receptors, suggesting high potency. It also shows noteworthy affinities for Alpha-2A (13.4 nM) and Alpha-2C (7.9 nM) receptors, along with rat Alpha-2B adrenergic receptor (6.8 nM). In various assays, Tamsulosin demonstrated powerful in vitro antagonism, particularly against human Alpha-1A, Alpha-1B, and Alpha-1D adrenergic receptors with further confirmation of its in vivo efficacy in an intraurethral pressure model in aged anesthetized dogs (Kd = 1.349 nM) and a spontaneously hypertensive rat model (pED50 = 7.33). The compound also exhibited inhibition of A61603-induced contraction in rats with an AD50 of 3.0 µg/kg, maintaining efficacy over 3.5 hours. Furthermore, Tamsulosin showed high affinity for human cloned Alpha-1A, Alpha-1B, and Alpha-1D receptors, with Ki values of 0.19 nM, 2.0 nM, and 0.2 nM, respectively. In pharmacokinetic evaluations, Tamsulosin displayed high oral bioavailability (Fa = 1.0), efficient evasion of hepatic elimination (Fh = 0.98), and moderate clearance rates (CL = 0.62 mL/min/kg). It exhibited a half-life of 6.8 hours in humans post-intravenous administration and a low fraction unbound (Fu = 0.01), with a steady-state volume of distribution (Vdss) of 0.21 L/kg, indicating extensive distribution across body tissues. Notably, there was no evidence of liver toxicity (DILI severity class of 0.0). Moreover, Tamsulosin possesses antagonistic activity on Alpha-1A, Alpha-1B, and Alpha-1D adrenoceptors, which is demonstrated through various IC50 values, supporting its potential in modulating adrenergic signaling pathways. In antiviral assessments, although weak against SARS-CoV-2 (hit score 0.1193), it showed 22.04% inhibition of the SARS-CoV-2 3CL-Pro protease at 20 µM concentration. The compound also illustrated a degree of enzymatic inhibition, targeting human HDAC6 and MAOA, among other enzymes. These collective pharmacological characteristics suggest Tamsulosin as a promising candidate for therapeutic applications involving adrenergic receptor modulation, with a broad spectrum of potential bioactivities..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Tamsulosin ((R)-(-)-YM12617 free base) is an alpha1A adrenergic receptor antagonist used for the symptomatic treatment of benign prostatic hyperplasia (BPH). It treats difficulty urinating, a common symptom of an enlarged prostate, by relaxing the neck muscles of the bladder and muscle fibers in the prostate itself, easing urination.
Synonyms	LY253351 free base, HSDB-7744, HSDB7744, HSDB 7744, Harnal-D, Flowmax, (R)-(-)-YM12617 free base

Chemical Properties

Molecular Weight	408.51
Formula	C₂₀H₂₈N₂O₅S
Cas No.	106133-20-4
Smiles	CCOc1ccccc1OCCN[C@H](C)Cc1ccc(OC)c(c1)S(N)(=O)=O
Relative Density.	1.191 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (611.98 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (8.08 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4479 mL	12.2396 mL	24.4792 mL	122.3960 mL
5 mM	0.4896 mL	2.4479 mL	4.8958 mL	24.4792 mL
10 mM	0.2448 mL	1.2240 mL	2.4479 mL	12.2396 mL
20 mM	0.1224 mL	0.6120 mL	1.2240 mL	6.1198 mL
50 mM	0.0490 mL	0.2448 mL	0.4896 mL	2.4479 mL
100 mM	0.0245 mL	0.1224 mL	0.2448 mL	1.2240 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc