Silodosin

Catalog No.S1613 Synonyms: KAD 3213, KMD 3213

For research use only.

Silodosin (KAD 3213, KMD 3213) is a highly selective α1A-adrenoceptor antagonist, used in treatment of benign prostatic hyperplasia.

Silodosin Chemical Structure

CAS No. 160970-54-7

Purity & Quality Control

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Biological Activity

Description Silodosin (KAD 3213, KMD 3213) is a highly selective α1A-adrenoceptor antagonist, used in treatment of benign prostatic hyperplasia.
Targets
α1-adrenergic receptor [1]
In vitro

Silodosin shows higher selectivity for the alpha(1A)-AR subtype than tamsulosin hydrochloride, naftopidil or prazosin hydrochloride (affinity is highest for tamsulosin hydrochloride, followed by silodosin, prazosin hydrochloride and naftopidil in that order). [1] Silodosin and tadalafil have synergistic inhibitor effects on nerve-mediated contractions of human and rat isolated prostates in rats. [2]

In vivo Silodosin strongly antagonizes noradrenaline-induced contractions in rabbit lower urinary tract tissues (including prostate, urethra and bladder trigone, with pA(2) or pKb values of 9.60, 8.71 and 9.35, respectively). [1] Silodosin significantly inhibits the phenylephrine-induced increase in intraurethral pressure (versus the vehicle-treated group) at 12 hours, 18 hours, and 24 hours after its oral administration in rats. [3] Silodosin (0.1-0.3 mg/kg) or prazosin (0.03-0.1 mg/kg) reduces obstruction-induced increases in intraluminal ureter pressures by 21-37% or 18-40% respectively. Silodosin inhibits contractions of the rat and human isolated ureters and has excellent functional selectivity in vivo to relieve pressure-load of the rat obstructed ureter. [4] Silodosin (0.3-300 mg/kg) dose-dependently inhibits the hypogastric nerve stimulation-induced increase in intraurethral pressure (without significant hypotensive effects) in both young and old dogs with benign prostatic hyperplasia. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 495.53
Formula

C25H32F3N3O4

CAS No. 160970-54-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(CC1=CC2=C(C(=C1)C(=O)N)N(CC2)CCCO)NCCOC3=CC=CC=C3OCC(F)(F)F

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01757769 Completed Drug: Silodosin Benign Prostatic Hyperplasia RECORDATI GROUP May 2011 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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