Oxymetazoline HCl

Alias: Oxylazine; Rhinofrenol; Afrin; Ocuclear; Drixine; Nezeril; Sinerol; Hazol; Nafrine; Navasin; oxymeta zoline; Ocuclear

Cat No.:V1115 Purity: ≥98%

COA Product Data Instructions for use SDS

Oxymetazoline HCl Chemical Structure CAS No.: 2315-02-8
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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Citations by Top Journals: Nature, Cell, Science, etc.

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.

Cell Reports 2023,42(4):112313

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

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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

Product Description

Oxymetazoline HCl (Rhinofrenol; Afrin; Ocuclear; Drixine; Nezeril; Sinerol; Hazol; Nafrine; Navasin), the hydrochloride salt of oxymetazoline, is an imidazole-based α1 and α2 adrenergic receptor agonist. It is a topical decongestant that has been primarily used to treat hay fever, allergies, and cold-related nasal discomfort. When it comes to alpha 1a subtype, oxymetazoline has higher affinities than alpha 1b and alpha 1d subtypes. With regard to the other subtypes of alpha 1a-adrenoceptors, oxymetazoline exhibits no intrinsic activity and is only a weak agonist. At the 5-HT1A, 5-HT1B, and 5-HT1D receptors, oxymetazoline is a complete and potent agonist; at the 5-HT1C receptor, it is a partial agonist.

Biological Activity I Assay Protocols (From Reference)

ln Vitro

In vitro activity: Oxymetazoline possesses greater affinity for the alpha 1a subtype than the alpha 1b and alpha 1d subtypes. With regard to alpha 1a-adrenoceptors, oxymetazoline is a weak agonist with no intrinsic activity at the other subtypes. At 5-HT1A, 5-HT1B, and 5-HT1D receptors, oxymetazoline is a complete and potent agonist; at 5-HT1C receptors, it is a partial agonist. In a cell-free system, oxymetazoline (0.4–1 mM) does not change the oxidation of methionine caused by ultrafine carbon particles (UCPs) and inhibits the activity of 5-lipoxygenase (5-LO) but not 15-lipoxygenase (15-LO). In canine alveolar macrophages (AMs), oxymetazoline strongly inhibits eukotriene B(4) (LTB(4)) and respiratory burst at 0.4/0.1 mM (p < 0.05), increases prostaglandin E(2) (PGE(2)) at 0.1 mM, and induces phospholipase A(2) (PLA(2)) activity and 15(S)-hydroxy-eicosatetraenoic acid (15-HETE) at 1 mM. However, it has no effect on 8-isoprostane formation. Oxymetazoline inhibits the formation of LTB(4) at 0.1 mM, respiratory burst at 0.001 mM, and 8-isoprostane at 0.1 mM induced by UCP. In canine alveolar macrophages (AMs), oxymetazoline inhibits proinflammatory responses such as 5-LO activity, LTB(4) formation, and respiratory burst and stops particle-induced oxidative stress. In cultured rabbit nonpigmented ciliary epithelial cells and rabbit iris-ciliary bodies, isoproterenol-stimulated cAMP production is inhibited by oxymetazoline. By activating ciliary epithelium's alpha 2A receptors, oxymetazoline reduces intraocular pressure; this ocular hypotensive effect is not entirely reliant on intact sympathetic nerves.

ln Vivo

Animal Protocol

References

[1]. Br J Pharmacol . 1995 Sep;116(1):1611-8.

[2]. Eur J Pharmacol . 1991 Apr 17;196(2):213-6.

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

Physicochemical Properties

Molecular Formula

C16H25CLN2O

Molecular Weight

296.84

Exact Mass

260.17

Elemental Analysis

C, 64.74; H, 8.49; Cl, 11.94; N, 9.44; O, 5.39

CAS #

2315-02-8

Related CAS #

1491-59-4 (free); 2315-02-8 (HCl)

Appearance

White to off-white crystalline powder

SMILES

CC1=CC(=C(C(=C1CC2=NCCN2)C)O)C(C)(C)C.Cl

InChi Key

BEEDODBODQVSIM-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H24N2O.ClH/c1-10-8-13(16(3,4)5)15(19)11(2)12(10)9-14-17-6-7-18-14;/h8,19H,6-7,9H2,1-5H3,(H,17,18);1H

Chemical Name

6-tert-butyl-3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethylphenol;hydrochloride

Synonyms

Oxylazine; Rhinofrenol; Afrin; Ocuclear; Drixine; Nezeril; Sinerol; Hazol; Nafrine; Navasin; oxymeta zoline; Ocuclear

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: ~59 mg/mL (~198.7 mM)

Water: ~59 mg/mL (~198.7 mM)

Ethanol: N/A

Solubility (In Vivo)

Chemical Name:6-tert-butyl-3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethylphenol hydrochloride

InChi Key:BEEDODBODQVSIM-UHFFFAOYSA-N

InChi Code:InChI=1S/C16H24N2O.ClH/c1-10-8-13(16(3,4)5)15(19)11(2)12(10)9-14-17-6-7-18-14;/h8,19H,6-7,9H2,1-5H3,(H,17,18);1H

SMILES Code:OC1=C(C(C)(C)C)C=C(C)C(CC2=NCCN2)=C1C.[H]Cl

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.3688 mL	16.8441 mL	33.6882 mL
	5 mM	0.6738 mL	3.3688 mL	6.7376 mL
	10 mM	0.3369 mL	1.6844 mL	3.3688 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

Calculate Reset

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
NCT03529487	Active Recruiting	Drug: Oxymetazoline	Fecal Incontinence	RDD Pharma Ltd	August 20, 2018	Phase 1
NCT02630121	Recruiting	Drug: Oxymetazoline Hydrochloride Drug: Placebo	Sleep Apnea Chronic Nasal Congestion	University of South Florida	April 2023	Phase 4
NCT05945615	Not yet recruiting	Drug: Oxymetazoline 0.1% (Pf) Oph Soln Ud Other: Preservative free lubricating drops	Blepharoptosis Synkinesis	Milton S. Hershey Medical Center	January 2024	Phase 3
NCT05348148	Recruiting	Drug: Oral Levocetirizine Drug: Combined Intranasal Mometasone Furoate with oral Levocetirizine	Allergic Rhinitis Vasomotor Rhinitis	Camillians Saint Mary's Hospital Luodong	June 16, 2020	Not Applicable
NCT04153188	Completed	Device: The Vbeam® Prima System Drug: Oxymetazoline HCL 1% Cream	Erythematotelangiectatic Rosacea	Candela Corporation	January 15, 2019	Phase 4