1. GPCR/G Protein Neuronal Signaling Anti-infection
  2. Adrenergic Receptor Bacterial
  3. Silodosin

Silodosin  (Synonyms: KAD 3213; KMD 3213)

Cat. No.: HY-10122 Purity: 99.85%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Silodosin Chemical Structure

Silodosin Chemical Structure

CAS No. : 160970-54-7

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

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Description

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[1][3].

IC50 & Target

Ki: 0.036 nM (α1A-AR); 21 nM (α1B-AR); 2 nM (α1D-AR)[1]

In Vitro

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[1].
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[2].
Silodosin (0-10 µM; 24 hours) decreases ELK1 gene expression as a dose-dependent manner in all the bladder cancer cell lines[4].
Silodosin (0-10 µM; 24 hours) decreases ELK1 protein expression as a as a dose-dependent manner[4].
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)[4].

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

RT-PCR[4]

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[4]

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[4]

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).
In Vivo

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[2].

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

Animal Model: Sprague Dawley rats[2]
Dosage: 0.1-0.3mg/kg
Administration: Intravenous injection
Result: Effectively reduced contractions of both human and rat isolated ureters.
Clinical Trial
Molecular Weight

495.53

Formula

C25H32F3N3O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)C1=CC(C[C@@H](C)NCCOC2=CC=CC=C2OCC(F)(F)F)=CC3=C1N(CC3)CCCO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (100.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (5.05 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.05 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.85%

References

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 2.0180 mL 10.0902 mL 20.1804 mL 50.4510 mL
5 mM 0.4036 mL 2.0180 mL 4.0361 mL 10.0902 mL
10 mM 0.2018 mL 1.0090 mL 2.0180 mL 5.0451 mL
15 mM 0.1345 mL 0.6727 mL 1.3454 mL 3.3634 mL
20 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5226 mL
25 mM 0.0807 mL 0.4036 mL 0.8072 mL 2.0180 mL
30 mM 0.0673 mL 0.3363 mL 0.6727 mL 1.6817 mL
40 mM 0.0505 mL 0.2523 mL 0.5045 mL 1.2613 mL
50 mM 0.0404 mL 0.2018 mL 0.4036 mL 1.0090 mL
60 mM 0.0336 mL 0.1682 mL 0.3363 mL 0.8409 mL
80 mM 0.0252 mL 0.1261 mL 0.2523 mL 0.6306 mL
100 mM 0.0202 mL 0.1009 mL 0.2018 mL 0.5045 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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