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Xylometazoline HCl

Alias: xylomethazoline; Xylometazoline HCl; Brand name: Decongest; Otrivine; Balkis; Amidrin; Chlorohist-LA; espa-rhin; Gelonasal
Cat No.:V1125 Purity: ≥98%
Xylometazoline HCl (xylomethazoline; Otrivine; Amidrin; Balkis; Chlorohist-LA; Decongest; espa-rhin; Gelonasal),the hydrochloride salt of Xylometazoline, is an α-adrenoceptor agonist commonly used as nasal decongestant.
Xylometazoline HCl
Xylometazoline HCl Chemical Structure CAS No.: 1218-35-5
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
10g
25g
Other Sizes

Other Forms of Xylometazoline HCl:

  • Xylometazoline
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Xylometazoline HCl (xylomethazoline; Otrivine; Amidrin; Balkis; Chlorohist-LA; Decongest; espa-rhin; Gelonasal), the hydrochloride salt of Xylometazoline, is an α-adrenoceptor agonist commonly used as nasal decongestant.shows maximum potency at the α2B-adrenoceptor subtype with EC50 of 99 μM. Xylometazoline, a α-adrenoceptor agonist that is frequently used as a nasal decongestant, has an EC50 of 99 μM and is most potent at the α2B-adrenoceptor subtype. With an IC50 of 0.08, 0.56, 0.45, 0.98, 1.8, and 0.22 μM, respectively, xylometazoline binds at adrenoceptor subtypes α1A, α1B, α1D, α2A, α2B, and α2C.

Biological Activity I Assay Protocols (From Reference)
Targets
Alpha-1A adrenergic receptor ( Ki = 0.05 μM ); Alpha-1B adrenergic receptor ( Ki = 0.30 μM ); Alpha-1D adrenergic receptor ( Ki = 0.15 μM ); Alpha-2A adrenergic receptor ( Ki = 0.88 μM ); Alpha-2B adrenergic receptor ( Ki = 1.7 μM ); Alpha-2C adrenergic receptor ( Ki = 0.19 μM nM )
ln Vitro

In vitro activity: Xylometazoline, an α-adrenoceptor agonist that is frequently used as a nasal decongestant, has the highest potency at the α2B-adrenoceptor subtype with EC50 of 99 μM. At adrenoceptor subtypes α1A, α1B, α1D, α2A, α2B, and α2C, xylometazoline binds with IC50 values of 0.08, 0.56, 0.45, 0.98, 1.8, and 0.22μM, respectively.[1]

ln Vivo

Animal Protocol


ADME/Pharmacokinetics
Absorption, Distribution and Excretion
No information is available on xylometazoline pharmacokinetics.
No information is available on xylometazoline pharmacokinetics.
No information is available on xylometazoline pharmacokinetics.
No information is available on xylometazoline pharmacokinetics.
Metabolism / Metabolites
No information is available on xylometazoline pharmacokinetics.
Biological Half-Life
No information is available on xylometazoline pharmacokinetics.
Toxicity/Toxicokinetics
Protein Binding
No information is available on xylometazoline pharmacokinetics.
References

[1]. Fundam Clin Pharmacol . 2010 Dec;24(6):729-39.

Additional Infomation
Xylometazoline is an alkylbenzene.
Xylometazoline is an imidazoline derivative with sympathomimetic and nasal decongestant activity. Xylometazoline works by binding to alpha (α)-adrenergic receptors to cause vasoconstriction of nasal blood vessels. Xylometazoline is available in over-the-counter (OTC) nasal sprays or drops to temporarily relieve nasal congestion due to cold, hay fever or other respiratory allergies. In some countries, it is available as combination products with [ipratropium], [domiphen], or [dexpanthenol].
See also: Xylometazoline Hydrochloride (has salt form).
Drug Indication
Xylometazoline is indicated for the temporary relief of nasal congestion due to cold, hay fever or other respiratory allergies.
Mechanism of Action
Nasal congestion is caused by various etiologies, such as rhinosinusitis and allergic or non-allergic rhinitis, leading to congestion of the venous sinusoids lining the nasal mucosa. Activation of α-adrenergic receptors leads to vasoconstriction of the blood vessels of the nasal mucosa and resumption of nasal airflow. As the most abundantly expressed in the human nasal mucosa, α1A- and α2B-adrenoceptors may play the most important role in vasoconstriction of the human nasal mucosa. Xylometazoline is a more selective agonist at α2B-adrenoceptors, with affinity at α1A-, α2A-, α2C-, α1B-, and α1D-adrenoceptors. Xylometazoline decreases nasal resistance during inspiration and expiration and increases the volume of nasal airflow. Compared to [oxymetazoline], another imidazoline nasal decongestant, xylometazoline had a slightly faster onset of action although they had a similar duration of action. In one study, subjects with nasal congestion reported relief of earache and sore throat in addition to nasal decongestion: it is speculated that oxymetazoline mediates this effect by causing vasoconstriction of the nasal mucosa that contains the venous sinuses and nasal decongestion allows breathing through the nose, providing relief from sore throat caused by mouth breathing that dries and irritates the throat.
Pharmacodynamics
Xylometazoline is a sympathomimetic agent that causes vasoconstriction of the nasal mucosa. In one study comprising subjects with nasal congestion associated with the common cold, the median time of onset of subjective relief of nasal congestion was about 1.7 minutes and the time of subjective peak relief of nasal congestion was 30 minutes. Previous studies reported rebound swelling, rebound nasal congestion, rhinitis medicamentosa, and shorter duration of decongestant effect from the long-term use of xylometazoline in healthy volunteers, suggesting that the drug is most effective if used temporarily. An early _in vitro_ study demonstrated xylometazoline to exert anti-oxidant actions, where it inhibited microsomal lipid peroxidation and mediated hydroxyl radical scavenging activity. This suggests that xylometazoline has a beneficial effect against oxidants, which play a role in tissue damage in inflammation.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H25CLN2
Molecular Weight
280.84
Exact Mass
280.17
Elemental Analysis
C, 68.43; H, 8.97; Cl, 12.62; N, 9.98
CAS #
1218-35-5
Related CAS #
Xylometazoline; 526-36-3
PubChem CID
5709
Appearance
White to off-white crystalline powder
Boiling Point
394.2ºC at 760 mmHg
Melting Point
131-133ºC
Flash Point
192.2ºC
Vapour Pressure
4.56E-06mmHg at 25°C
LogP
3.711
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
1
Rotatable Bond Count
3
Heavy Atom Count
18
Complexity
302
Defined Atom Stereocenter Count
0
SMILES
Cl[H].N1([H])C([H])([H])C([H])([H])N=C1C([H])([H])C1C(C([H])([H])[H])=C([H])C(=C([H])C=1C([H])([H])[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
InChi Key
YGWFCQYETHJKNX-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H24N2.ClH/c1-11-8-13(16(3,4)5)9-12(2)14(11)10-15-17-6-7-18-15;/h8-9H,6-7,10H2,1-5H3,(H,17,18);1H
Chemical Name
2-[(4-tert-butyl-2,6-dimethylphenyl)methyl]-4,5-dihydro-1H-imidazole;hydrochloride
Synonyms
xylomethazoline; Xylometazoline HCl; Brand name: Decongest; Otrivine; Balkis; Amidrin; Chlorohist-LA; espa-rhin; Gelonasal
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: 25~27 mg/mL (89.0~96.1 mM)
Water: ~56 mg/mL (~199.4 mM)
Ethanol: ~56 mg/mL (~199.4 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.90 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 25.0 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: ≥ 2.5 mg/mL (8.90 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 25.0 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: ≥ 2.5 mg/mL (8.90 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 16.67 mg/mL (59.36 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.5607 mL 17.8037 mL 35.6075 mL
5 mM 0.7121 mL 3.5607 mL 7.1215 mL
10 mM 0.3561 mL 1.7804 mL 3.5607 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:
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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
NCT05334017 Completed Drug: Xylometazoline 0,1%
Drug: Cocaine 4%
Epistaxis Rigshospitalet, Denmark September 8, 2022 Phase 4
NCT03424889 Completed Drug: Xylometazoline
Drug: Saline
Bronchoscopy All India Institute of Medical
Sciences, New Delhi
June 1, 2018 Not Applicable
NCT00452270 Completed Drug: Xylometazoline Common Cold Novartis March 2007 Phase 3
NCT00622817 Completed Drug: xylometazoline HCL 0.05%
Drug: Epinephrine 1mg
Bronchiolitis Schneider Children's Medical
Center, Israel
October 2004 Not Applicable
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