Tamsulosin
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.80%
- CAS. Nr.: 106133-20-4
- Formel: C20H28N2O5S
- Molecular Weight:408.51
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tamsulosin
MoreAlle Adrenergic Receptor Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
α1-adrenergic receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
0.13 nM
Compound: Tamsulosin
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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
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[PMID: 27658792] |
| HEK293 | IC50 |
1.4 nM
Compound: 1
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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
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[PMID: 27709945] |
| HEK293 | IC50 |
2.2 nM
Compound: 1
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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
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[PMID: 27709945] |
| HEK293 | IC50 |
4.8 nM
Compound: 1
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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
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[PMID: 27709945] |
In Vitro
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].
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Tamsulosin (50-400 μM, 24 h) induces apoptosis and clusterin expression in NRP-152 cells[5].
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MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human glomerular endothelial cells (GECs)
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Concentration:25, and 50 nM
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Incubation Time:24 h
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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.
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Cell Line:Human glomerular endothelial cells (GECs)
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Concentration:25, and 50 nM
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Incubation Time:24 h
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Result:Decreased nuclear NF-κB p65 to 2.7- and 1.9- fold at 25 and 50 nM, respectively.
In Vivo
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.
Chemical Information
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CAS. Nr. 106133-20-4
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Appearance Solid
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Molecular Weight 408.51
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Formel C20H28N2O5S
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Color White to off-white
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SMILES
O=S(C1=CC(C[C@H](NCCOC2=CC=CC=C2OCC)C)=CC=C1OC)(N)=O
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Synonyms
(R)-(-)-YM12617 free base; LY253351 free base
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
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
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Most Recent
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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
Lösungsmittel & Löslichkeit
In Vitro:
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Tamsulosin Related Classifications
HY-B0661 Related Classifications
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