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Alfuzosin HCl (SL 77499-10 HCl)

Alias:
Cat No.:V1099 Purity: ≥98%
Alfuzosin HCl (Alfetim; alfusozine; SL-77499; alphuzosine; Benestan; Urion; UroXatral; Xatral), the hydrochloride salt of alfuzosin, is an approved/marketed drug which acts as an alpha1 adrenergic receptor antagonist.
Alfuzosin HCl (SL 77499-10 HCl)
Alfuzosin HCl (SL 77499-10 HCl) Chemical Structure CAS No.: 81403-68-1
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Alfuzosin HCl (SL 77499-10 HCl):

  • Alfuzosin (SL 77499)
  • Alfuzosin-d7 hydrochloride (SL 77499-10-d7)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Alfuzosin HCl (Alfetim; alfusozine; SL-77499; alphuzosine; Benestan; Urion; UroXatral; Xatral), the hydrochloride salt of alfuzosin, is an approved/marketed drug which acts as an alpha1 adrenergic receptor antagonist. It is authorized for use in the management of BPH, or benign prostatic hyperplasia.

Biological Activity I Assay Protocols (From Reference)
Targets
α1-adrenergic receptor
ln Vitro

In vitro activity: Alfuzosin increases the probability of late hNa(v)1.5 single-channel openings, significantly reduces the slow time constant for recovery from inactivation, and increases whole-cell peak sodium (hNa(v)1.5) current. Alfuzosin also causes a 2- to 3-fold increase in the length of the hNa(v)1.5 burst and the number of openings per burst.[1] When 10 mM phenylephrine is used to pre-contract the rabbit corpus cavernosum (CC), alfuzosin exhibits a concentration-dependent relaxing effect.[2]

ln Vivo
Alfuzosin (300 nM) dramatically lengthens the action potential duration (APD)(60) and QT in isolated rabbit hearts.[1] Alfuzosin increases the quantity and size of apomorphine-induced erections in spontaneously hypertensive rats (SHR).[3] Alfuzosin functions as an antagonist of the alpha-adrenergic receptor, preventing contractions brought on by external noradrenaline while leaving the spikes in the two vas deferens segments unchanged.[4] In the pithed rat, alfuzosin (0.03-0.3 mg kg-1, i.v.) significantly suppresses pressor responses elicited by the alpha 1-selective agonist Cirazoline, but it only marginally suppresses responses to the alpha 2-selective agonist UK 14,304. When it comes to responses mediated by activation of prejunctional alpha 2-receptors, alfuzosin (1 mg kg-1, i.v.) has negligible effects (UK 14,304-induced inhibition of sympathetic tachycardia). In the cat under anesthesia, alfuzosin (0.001–1 mg kg–1, intravenously) and prazosin (0.001-0.3 mg kg–1, intravenously) produce dose-related inhibition of the increases in urethral pressure brought on by stimulation of sympathetic hypogastric nerves. [5]
Animal Protocol
0.001-1 mg kg-1, i.v.
Rats amd cats
References

[1]. J Pharmacol Exp Ther . 2008 Feb;324(2):427-33.

[2]. BJU Int . 2003 Jun;91(9):873-7.

[3]. Eur Urol . 2004 Jan;45(1):110-6; discussion 116.

[4]. J Pharmacol Exp Ther . 2005 Feb;312(2):710-7.

[5]. Br J Pharmacol . 1993 Aug;109(4):1282-9.

Additional Infomation
Alfuzosin Hydrochloride is the hydrochloride salt of alfuzosin, a quinazoline compound with smooth muscle-relaxing activity. Alfuzosin selectively binds to and antagonizes post-synaptic alpha-1-adrenoreceptors in smooth muscle of the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra, initiating relaxation of smooth muscle and resulting in improvement of urine flow and the symptoms of benign prostatic hyperplasia (BPH). This agent also blocks alpha-1-adrenoreceptors in peripheral vascular smooth muscle, resulting in vasodilatation and a decrease in peripheral vascular resistance.
See also: Alfuzosin (has active moiety).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H28CLN5O4
Molecular Weight
425.91
Exact Mass
425.182
Elemental Analysis
C, 58.60; H, 6.99; N, 17.98; O, 16.43
CAS #
81403-68-1
Related CAS #
Alfuzosin; 81403-80-7; Alfuzosin-d7 hydrochloride; 1276197-14-8
PubChem CID
71764
Appearance
White to off-white solid powder
Density
1.272 g/cm3
Boiling Point
687.7ºC at 760 mmHg
Melting Point
225°C
LogP
3.124
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
8
Heavy Atom Count
29
Complexity
511
Defined Atom Stereocenter Count
0
SMILES
Cl.O=C(C1CCCO1)NCCCN(C)C1N=C2C(C=C(C(=C2)OC)OC)=C(N)N=1
InChi Key
YTNKWDJILNVLGX-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H27N5O4.ClH/c1-24(8-5-7-21-18(25)14-6-4-9-28-14)19-22-13-11-16(27-3)15(26-2)10-12(13)17(20)23-19;/h10-11,14H,4-9H2,1-3H3,(H,21,25)(H2,20,22,23);1H
Chemical Name
N-[3-[(4-amino-6,7-dimethoxyquinazolin-2-yl)-methylamino]propyl]oxolane-2-carboxamide;hydrochloride
Synonyms

SL-77499; Alfetim; alfusozine; alfuzosin; SL 77499; SL77499; alfuzosin hydrochloride; alphuzosine; Benestan; Urion; UroXatral; Xatral

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

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 25~85 mg/mL (58.7~199.6 mM)
Water: ~85 mg/mL (~199.6 mM)
Ethanol: ~85 mg/mL (~199.6 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.88 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 20.8 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: ≥ 2.08 mg/mL (4.88 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 20.8 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.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (4.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3479 mL 11.7396 mL 23.4791 mL
5 mM 0.4696 mL 2.3479 mL 4.6958 mL
10 mM 0.2348 mL 1.1740 mL 2.3479 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00576823 Completed Drug: Alfuzosin Neurogenic Bladder
Hydronephrosis
Sanofi December 2007 Phase 3
NCT00696761 Completed Drug: Alfuzosin BPH Asan Medical Center May 2006 Phase 4
NCT00893113 Completed Drug: Alfuzosin
Drug: Placebo
Lower Urinary Tract Symptoms
Erectile Dysfunction
Chesapeake Urology Research
Associates
June 2009 Phase 3
NCT00575913 Completed Drug: Alfuzosin Prostatic Diseases Sanofi September 2003 Phase 4
NCT02266537 Completed Drug: Alfuzosin
Drug: Doxazosin
Healthy Boehringer Ingelheim November 2005 Phase 1
Biological Data
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