1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. Silodosin

Silodosin (Synonyms: KAD 3213; KMD 3213)

Cat. No.: HY-10122 Purity: 99.96%
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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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 108 In-stock
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100 mg USD 162 In-stock
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Based on 1 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].

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].

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.
SMILES

O=C(N)C1=CC(C[[email protected]@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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (100.90 mM)

*"≥" 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
10 mM 0.2018 mL 1.0090 mL 2.0180 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.05 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.96%

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Keywords:

SilodosinKAD 3213 KMD 3213KAD3213KAD-3213KMD3213KMD 3213KMD-3213Adrenergic ReceptorBeta ReceptorLUTSlowerurinarytractsymptomsBPHbenignprostatichyperplasiacancerInhibitorinhibitorinhibit

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Silodosin
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