Silodosin (KAD 3213; KMD 3213)

Alias: KAD 3213; KMD 3213; KMD 3213; KAD 3213; KMD-3213; KMD3213; KAD 3213; KAD3213; Silodosin; trade names: Rapaflo; Silodyx, Rapilif; Silodal; Urief; Urorec
Cat No.:V1111 Purity: ≥98%
ilodosin (KMD-3213; KMD3213; KAD3213; KAD-3213; Silodosin; trade names Rapaflo, Silodal, Silodyx, Rapilif, Urief, Urorec) is a highly selective alpha1A/α1A-adrenoceptor antagonist that was approved for the treatment of BPH-benign prostatic hyperplasia.
Silodosin (KAD 3213; KMD 3213) Chemical Structure CAS No.: 160970-54-7
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
25mg
50mg
100mg
250mg
500mg
1g
2g
5g
Other Sizes

Other Forms of Silodosin (KAD 3213; KMD 3213):

  • Silodosin-d4 (silodosin d4)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Silodosin (KMD-3213; KMD3213; KAD3213; KAD-3213; Silodosin; trade names Rapaflo, Silodal, Silodyx, Rapilif, Urief, Urorec) is a highly selective alpha1A/α1A-adrenoceptor antagonist that was approved for the treatment of BPH-benign prostatic hyperplasia.

Biological Activity I Assay Protocols (From Reference)
Targets
α1A-AR ( Ki = 0.036 nM ); α1B-AR ( Ki = 21 nM ); α1D-AR ( Ki = 2 nM )
ln Vitro

In vitro activity: Silodosin (KAD 3213; KMD 3213) has a much weaker inhibitory effect on the alpha 1b- and alpha 1d-ARs, but it can inhibit norepinephrine-induced increases in intracellular Ca2+ concentrations in Chinese hamster ovary cells expressing alpha 1a-AR with an IC50 of 0.32 nM[1]. Silodosin has a Ki value of 0.036 nM and potently inhibits the binding of 2-[2-(4-hydroxy-3-[125I]iodophenyl)ethylaminomethyl]-alpha-tetralone to the cloned human alpha 1a-AR, but its potency is 56- and 583-fold lower at the alpha 1b- and alpha 1d-ARs, respectively[2]. Silodosin (0–10 µM; 24 hours) reduces ELK1 gene expression in a dose-dependent manner in all the bladder cancer cell lines[4]. (0–10 µM; 24 hours) reduces the expression of the ELK1 protein in a dose-dependent manner[4]. Silodosin (0-10 µM; 96 hours) barely affects the cell viability of AR-negative 647V or AR-positive UMUC3 or TCCSUP grown in an androgen-depleted environment. On the other hand, silodosin inhibited the growth of UMUC3 cells grown in normal FBS containing androgens (58% reduction at 10 µM)[4].

ln Vivo
Silodosin (intravenous injection; 0.1-0.3mg/kg) decreases the increases in MinP caused by obstruction by 20.7 percent (0.1 mg/kg) and 20.8 percent (0.3 mg/kg) respectively. For the treatment of LUTS/BPH, it may be useful for both storage and voiding dysfunction because it enhances detrusor overactivity and lowers the grade of obstruction[2].
Cell Assay
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
Animal Protocol
Sprague Dawley rats
0.1-0.3mg/kg
Intravenous injection
References

[1]. Silodosin in the treatment of benign prostatic hyperplasia. Drug Des Devel Ther. 2010; 4: 291–297.

[2]. Effects by silodosin on the partially obstructed rat ureter in vivo and on human and rat isolated ureters.Br J Pharmacol. 2013 May;169(1):230-8.

[3]. Silodosin : a new subtype selective alpha-1 antagonist for the treatment of lower urinary tract symptoms in patients with benign prostatic hyperplasia.Expert Opin Pharmacother. 2012 Oct;13(14):2085-96.

[4]. Silodosin inhibits the growth of bladder cancer cells and enhances the cytotoxic activity of cisplatin via ELK1 inactivation.Am J Cancer Res. 2015 Sep 15;5(10):2959-68. eCollection 2015.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H32F3N3O4
Molecular Weight
495.53
Exact Mass
495.23
Elemental Analysis
C, 60.60; H, 6.51; F, 11.50; N, 8.48; O, 12.91
CAS #
160970-54-7
Related CAS #
Silodosin-d4; 1426173-86-5
Appearance
Solid powder
SMILES
C[C@H](CC1=CC2=C(C(=C1)C(=O)N)N(CC2)CCCO)NCCOC3=CC=CC=C3OCC(F)(F)F
InChi Key
PNCPYILNMDWPEY-QGZVFWFLSA-N
InChi Code
InChI=1S/C25H32F3N3O4/c1-17(30-8-12-34-21-5-2-3-6-22(21)35-16-25(26,27)28)13-18-14-19-7-10-31(9-4-11-32)23(19)20(15-18)24(29)33/h2-3,5-6,14-15,17,30,32H,4,7-13,16H2,1H3,(H2,29,33)/t17-/m1/s1
Chemical Name
1-(3-hydroxypropyl)-5-[(2R)-2-[2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethylamino]propyl]-2,3-dihydroindole-7-carboxamide
Synonyms
KAD 3213; KMD 3213; KMD 3213; KAD 3213; KMD-3213; KMD3213; KAD 3213; KAD3213; Silodosin; trade names: Rapaflo; Silodyx, Rapilif; Silodal; Urief; Urorec
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~99 mg/mL (~199.8 mM)
Water: <1 mg/mL
Ethanol: ~99 mg/mL (~199.8 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (5.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05570084 Recruiting Drug: Silodosin
Drug: Tamsulosin
Stone, Urinary Princess Margaret Hospital,
Hong Kong
May 31, 2022 Phase 3
NCT05551221 Recruiting Drug: Silodosin Capsules
Drug: Ningmitai capsule
Benign Prostatic Hyperplasia
With Lower Urinary Tract
Symptoms
Xintian Pharmaceutical July 18, 2022 Phase 4
NCT05833386 Recruiting Procedure: Ureteral access
sheath placement during
flexible ureteroscope for
renal stones
Renal Stone Al-Azhar University October 1, 2022 Not Applicable
NCT06114979 Not yet recruiting Drug: Silodosin
Drug: Placebo
Lower Urinary Tract Symptoms Mansoura University November 1, 2023 Phase 3
NCT04107896 Completed Drug: Silodosin
Drug: Tamsulosin
Benign Prostatic Hyperplasia Bangabandhu Sheikh Mujib
Medical University, Dhaka,
Bangladesh
August 31, 2017 Phase 4
Biological Data
  • Effects of silodosin on ELK1 in bladder cancer cells. Am J Cancer Res . 2015 Sep 15;5(10):2959-68. eCollection 2015.
  • Effects of silodosin on bladder cancer cell growth. MTT assay in TCCSUP (A), UMUC3 (B, D), 647V (C), and UMUC3-ELK1-shRNA (E). Am J Cancer Res . 2015 Sep 15;5(10):2959-68. eCollection 2015.
  • Representative original ureteral pressure traces recorded after partial obstruction and administration of silodosin (A), tamsulosin (B) and prazosin (C) given at the maximal tested dose. Br J Pharmacol . 2013 May;169(1):230-8.
  • Ureter pressure parameters in vivo. Inhibitory effects of different doses of silodosin (black bars), tamsulosin (grey bars) or prazosin (white bars) on minimal (A) and maximal (B) ureter pressure, and AUC (C). Br J Pharmacol . 2013 May;169(1):230-8.
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