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Alfuzosin HCl Adrenergic Receptor antagonist

Cat.No.S1409

Alfuzosin HCI(SL 77499 HCl) is an alpha1 receptor antagonist used to treat benign prostatic hyperplasia (BPH).
Alfuzosin HCl  Adrenergic Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 425.91

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Quality Control

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (199.57 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 85 mg/mL

Ethanol : 85 mg/mL

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

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Chemical Information, Storage & Stability

Molecular Weight 425.91 Formula

C19H27N5O4.HCl

Storage (From the date of receipt)
CAS No. 81403-68-1 Download SDF Storage of Stock Solutions

Synonyms SL 77499 HCl Smiles CN(CCCNC(=O)C1CCCO1)C2=NC3=CC(=C(C=C3C(=N2)N)OC)OC.Cl

Mechanism of Action

Targets/IC50/Ki
α1-adrenergic receptor
In vitro

Alfuzosin significantly increases whole-cell peak sodium (hNa(v)1.5) current, increases the probability of late hNa(v)1.5 single-channel openings, and significantly shortens the slow time constant for recovery from inactivation. Alfuzosin also increases hNa(v)1.5 burst duration and number of openings per burst between 2- and 3-fold. Alfuzosin shows a concentration-dependent relaxing effect on rabbit corpus cavernosum (CC) pre-contracted by 10 mM phenylephrine.

In vivo

Alfuzosin (300 nM) significantly prolongs action potential duration (APD)(60) in rabbit Purkinje fibers and QT in isolated rabbit hearts. Alfuzosin enhances the number and amplitude of erections induced by apomorphine in spontaneous hypertensive rats (SHR). Alfuzosin behaves as an alpha-adrenergic antagonist blocking the contractions induced by exogenous noradrenaline without altering spikes in both portions of the vas deferens. Alfuzosin (0.03-0.3 mg kg-1, i.v.) markedly inhibits pressor responses produced by the alpha 1-selective agonist, Cirazoline but inhibits only slightly responses to the alpha 2-selective agonist, UK 14,304, in the pithed rat. Alfuzosin (1 mg kg-1, i.v.) has minimal effects against responses mediated by stimulation of prejunctional alpha 2-receptors (UK 14,304-induced inhibition of sympathetic tachycardia). Alfuzosin (0.001-1 mg kg-1, i.v.) and Prazosin (0.001-0.3 mg kg-1, i.v.) produces dose-related inhibition of the increases in urethral pressure caused by stimulation of sympathetic hypogastric nerves in the anaesthetized cat.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/15470085/
  • [5] https://pubmed.ncbi.nlm.nih.gov/8104650/

Clinical Trial Information

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

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06316336 Not yet recruiting
Healthy Vollunteer
Pharma Nueva
June 10 2024 Phase 1
NCT01685658 Withdrawn
Renal Colic|Acute Renal Colic
Centre Hospitalier Universitaire de Nīmes
September 2016 Phase 4
NCT00637715 Completed
Benign Prostatic Hyperplasia
Sanofi
October 2003 Phase 4
NCT00290030 Completed
Prostatic Hyperplasia|Acute Urinary Retention
Sanofi
May 2001 Phase 3

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