| Size | Price | Stock | Qty |
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| 2g |
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| 5g |
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| Other Sizes |
Purity: ≥98%
Tetrahydrozoline HCl (Tetryzoline; Tyzanol; Tyzine; Vasopos; Visine) is the hydrochloride salt of terazosin, which is an imidazoline-based alpha adrenergic receptor agonist with antihypertensive activity. It is an over-the-counter medication that comes in nasal spray and eye drop form.
| Targets |
α-adrenergic
α2-adrenergic receptor (Ki = 0.8 μM) [3] - α1-adrenergic receptor (weak affinity, Ki = 25 μM) [3] |
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| ln Vitro |
In vitro activity: Tetrahydrozoline hydrochloride (0.05% HCl-tetrahydrozoline diluted with DMEM to 1:20 concentration; 24 hours) stimulates primary human gingival fibroblasts to synthesize types I and III of collagen[3].
Treatment of primary human gingival fibroblasts with Tetrahydrozoline HCl (Tetryzoline) (0.1-10 μM) for 24 hours dose-dependently inhibited cell proliferation, with 10 μM reducing viability by 38% via MTT assay. Flow cytometry showed 18% apoptotic cells at 10 μM, accompanied by upregulated caspase-3 activity [3] - Tetrahydrozoline HCl (Tetryzoline) (1 μM) induced contraction of isolated human retinal microvascular smooth muscle cells by 42% compared to control, mediated via α2-adrenergic receptor activation [1] - In human gingival fibroblasts, Tetrahydrozoline HCl (Tetryzoline) (5 μM) downregulated collagen type I mRNA expression by 30% and MMP-2 mRNA expression by 25%, as detected by RT-PCR [3] |
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| ln Vivo |
Tetrahydrozoline HCl prevents Barnacle Balanus improvisus from settlin at 1μM.
Long-term topical application of Tetrahydrozoline HCl (Tetryzoline) (0.05% ophthalmic solution, twice daily) to human eyes for 2 years resulted in anterior segment vasculopathy (conjunctival vessel tortuosity, retinal capillary non-perfusion) and decreased visual acuity by 0.3 logMAR [1] - Intraperitoneal injection of Tetrahydrozoline HCl (Tetryzoline) (5 mg/kg) to mice increased systolic blood pressure by 20 mmHg within 10 minutes, lasting for 2 hours, via peripheral α2-adrenergic receptor-mediated vasoconstriction [3] |
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| Cell Assay |
Human gingival fibroblast proliferation and apoptosis assay: Primary human gingival fibroblasts were isolated and seeded in 96-well plates (3×10³ cells/well). Cells were treated with Tetrahydrozoline HCl (Tetryzoline) (0.1-10 μM) for 24 hours. Cell viability was measured by MTT assay. For apoptosis detection, cells were stained with Annexin V-FITC/PI and analyzed by flow cytometry. Caspase-3 activity was quantified using a colorimetric assay [3]
- Retinal microvascular smooth muscle contraction assay: Isolated human retinal microvascular smooth muscle cells were seeded in 24-well plates and cultured to confluence. Cells were treated with Tetrahydrozoline HCl (Tetryzoline) (0.1-10 μM) for 60 minutes. Cell contraction was assessed by measuring changes in cell surface area using image analysis software [1] |
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| Animal Protocol |
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| ADME/Pharmacokinetics |
After topical ophthalmic drops (0.05% solution), the systemic absorption by the human body is minimal, with a peak plasma concentration (Cmax) < 0.1 ng/mL [1]
- In the human body, tetrahydrozoline hydrochloride is mainly metabolized by oxidation in the liver, and 70% of the administered dose is excreted in the urine within 24 hours (20% as the original drug and 50% as metabolites) [2] - The elimination half-life (t1/2) of tetrahydrozoline hydrochloride in the human body is 3-4 hours [2] |
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| Toxicity/Toxicokinetics |
Long-term topical use of tetrahydrozoline hydrochloride (0.05% eye drops) is associated with ocular toxicity, including conjunctival hyperemia (12%), corneal epithelial damage (8%), and retinal vascular disease (rare, <1%) [1]
- 10 μM tetrahydrozoline hydrochloride induces mild cytotoxicity in human gingival fibroblasts, with a 22% increase in lactate dehydrogenase (LDH) release compared to the control group [3] - The median lethal dose (LD50) of tetrahydrozoline hydrochloride in mice via acute oral administration is 280 mg/kg [3] - Tetryzoline hydrochloride has a plasma protein binding rate of 35% in human plasma [2] |
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| References |
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| Additional Infomation |
Tetrahydrozoline hydrochloride is the hydrochloride salt of tetrahydrozoline. It is used as a nasal decongestant. It has the effects of a sympathomimetic, vasoconstrictor, and nasal decongestant. It contains the tetrahydrozoline (1+) ion. Tetrahydrozoline hydrochloride is the hydrochloride form of tetrahydrozoline, an imidazole derivative with sympathomimetic activity. When applied topically to the eyes or nose, tetrahydrozoline binds to and activates α-adrenergic receptors, thereby causing vasoconstriction and relieving nasal and eye congestion. See also: Tetrahydrozoline (containing active ingredient)... See more...
Tetrahydrozoline hydrochloride (tetrahydrozoline) is a direct-acting α-adrenergic receptor agonist with a higher affinity for α2 receptors than for α1 receptors[3] - Clinically, it is used as a topical ocular decongestant (0.05% solution) and nasal decongestant, exerting its effect through α2-adrenergic receptor-mediated conjunctival/nasal mucosal vasoconstriction[1,3] - Long-term or excessive use of Tetrahydrozoline hydrochloride (tetrahydrozoline) may lead to rebound congestion and ocular vascular lesions due to long-term vasoconstriction and receptor desensitization[1] - The drug can be detected in human blood and urine by gas chromatography-mass spectrometry (GC-MS), with a detection limit of 0.1 ng/mL in urine[2] |
| Molecular Formula |
C13H17CLN2
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| Molecular Weight |
236.74
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| Exact Mass |
236.108
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| Elemental Analysis |
C, 65.95; H, 7.24; Cl, 14.97; N, 11.83
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| CAS # |
522-48-5
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| Related CAS # |
Tetrahydrozoline; 84-22-0; Tetrahydrozoline-d4 hydrochloride; 1246814-66-3
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| PubChem CID |
10648
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| Appearance |
Solid powder
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| Boiling Point |
393.5ºC at 760 mmHg
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| Melting Point |
197 °C
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| Flash Point |
191.8ºC
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| LogP |
2.674
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
259
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].N1([H])C([H])([H])C([H])([H])N=C1C1([H])C2=C([H])C([H])=C([H])C([H])=C2C([H])([H])C([H])([H])C1([H])[H]
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| InChi Key |
BJORNXNYWNIWEY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H16N2.ClH/c1-2-6-11-10(4-1)5-3-7-12(11)13-14-8-9-15-13;/h1-2,4,6,12H,3,5,7-9H2,(H,14,15);1H
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| Chemical Name |
2-(1,2,3,4-tetrahydronaphthalen-1-yl)-4,5-dihydro-1H-imidazole;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| 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. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (7.05 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 16.7 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: ≥ 1.67 mg/mL (7.05 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 16.7 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. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (7.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (422.40 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2240 mL | 21.1202 mL | 42.2404 mL | |
| 5 mM | 0.8448 mL | 4.2240 mL | 8.4481 mL | |
| 10 mM | 0.4224 mL | 2.1120 mL | 4.2240 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.
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.
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