Size | Price | Stock | Qty |
---|---|---|---|
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
5g |
|
||
Other Sizes |
|
Purity: ≥98%
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.
Targets |
α1A-AR ( Ki = 0.036 nM ); α1B-AR ( Ki = 21 nM ); α1D-AR ( Ki = 2 nM )
|
|
---|---|---|
ln Vitro |
|
|
ln Vivo |
|
|
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 |
|
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 (In Vitro) |
|
|||
---|---|---|---|---|
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. View More
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. |
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.
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.
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 |
Effects of silodosin on ELK1 in bladder cancer cells. Am J Cancer Res . 2015 Sep 15;5(10):2959-68. eCollection 2015. td> |
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. td> |
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. td> |
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. td> |