Alfuzosin HCl (SL 77499-10 HCl)

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

Cat No.:V1099 Purity: ≥98%

COA Product Data Instructions for use SDS

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) 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.

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

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Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

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Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

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.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C19H28CLN5O4

Molecular Weight

425.91

Exact Mass

389.21

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

Appearance

Solid powder

SMILES

CN(CCCNC(=O)C1CCCO1)C2=NC3=CC(=C(C=C3C(=N2)N)OC)OC.Cl

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

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)

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

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

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

See Example

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.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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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

Molecular formula

Total molecular weight

g/mol

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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.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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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)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

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.)

% DMSO

% Tween 80

% ddH₂O

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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.

Note： (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

Alfuzosin delays cardiac repolarization.J Pharmacol Exp Ther.2008 Feb;324(2):427-33.
Alfuzosin prolongs QT.J Pharmacol Exp Ther.2008 Feb;324(2):427-33.
Alfuzosin increases opening probability of late cardiac sodium channels.J Pharmacol Exp Ther.2008 Feb;324(2):427-33.