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Silodosin

Name: Silodosin
Brand: Selleck Chemicals
SKU: S1613

Synonyms: KAD 3213, KMD 3213

Catalog No.S1613 Purity: 99.94%

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

Silodosin Chemical Structure

CAS: 160970-54-7

Purity & Quality Control

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

99.94

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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
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
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT01757769	Completed	Benign Prostatic Hyperplasia	RECORDATI GROUP	May 2011	Phase 4

References

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Chemical lnformation & Solubility

Molecular Weight	495.53	Formula	C₂₅H₃₂F₃N₃O₄
CAS No.	160970-54-7	SDF	Download Silodosin SDF
Smiles	CC(CC1=CC2=C(C(=C1)C(=O)N)N(CC2)CCCO)NCCOC3=CC=CC=C3OCC(F)(F)F
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 99 mg/mL ( (199.78 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 99 mg/mL

Water : Insoluble

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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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