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Silodosin Adrenergic Receptor antagonist

Cat.No.S1613

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

Chemical Structure

Molecular Weight: 495.53

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Quality Control

Batch: S161301 DMSO]99 mg/mL]false]Ethanol]99 mg/mL]false]Water]Insoluble]false Purity: 99.94%
99.94

Solubility

In vitro
Batch:

DMSO : 99 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 99 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 495.53 Formula

C25H32F3N3O4

Storage (From the date of receipt)
CAS No. 160970-54-7 Download SDF Storage of Stock Solutions

Synonyms KAD 3213, KMD 3213 Smiles CC(CC1=CC2=C(C(=C1)C(=O)N)N(CC2)CCCO)NCCOC3=CC=CC=C3OCC(F)(F)F

Mechanism of Action

Targets/IC50/Ki
α1-adrenergic receptor
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 this compound, prazosin hydrochloride and naftopidil in that order). This compound and tadalafil have synergistic inhibitor effects on nerve-mediated contractions of human and rat isolated prostates in rats.
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). This compound 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. It (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. This chemical 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. It (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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17052386/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19389393/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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