| Size | Price | Stock | Qty |
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| 5g |
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| 10g |
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| Other Sizes |
| Targets |
Bromhexine HCl targets mucus production and the TMPRSS2 protease. It acts as a mucolytic agent by breaking down mucus in the airways, making it easier to clear. It is also a potent and specific inhibitor of TMPRSS2, a protease involved in SARS-CoV-2 infection. By inhibiting TMPRSS2, it can prevent and manage SARS-CoV-2 infection. Bromhexine HCl is also an autophagy activator.
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| ln Vitro |
The natural expression of TMPRSS2 in LNCaP and C4-2B cells was dramatically inhibited by HGF-induced invasion when exposed to 250μM of bromhexine hydrochloride (BHH) for a 24-hour period [1]. When bromhexine hydrochloride was added to LNCaP, DU145, PC3, or HepG2 cells at doses ranging from 0 μM to 250 μM for 48 hours, no appreciable toxicity was seen. DU145 cell proliferation is not significantly inhibited or induced to die upon exposure to bromhexine hydrochloride [1]. HIV-1 infection of dendritic cells is inhibited by bromhexine hydrochloride (20 μM; 48 hours) [4].
In vitro, bromhexine HCl inhibits TMPRSS2 protease with an IC50 of 0.75 μM. It prevents and controls SARS-CoV-2 infection in cell-based assays. It is an autophagy activator. Its mucolytic activity has been demonstrated in various in vitro models. |
| ln Vivo |
In mice of the wild-type C57BL/6 strain, bromhexine hydrochloride (30 mg/kg; i.p.; three times weekly for five weeks) dramatically decreased the incidence of distant metastases to the liver and lungs from 55% in vehicle-treated animals to 20% in PIN (prostatic intraepithelial neoplasia) in TRAMP mice. Compared to TRAMP mice treated with vehicle, mice treated with bromhexine hydrochloride typically had prostates that were significantly bigger [1].
In vivo, bromhexine HCl is used for a variety of respiratory conditions associated with increased mucus secretion. It works by breaking down mucus in the airways, making it easier to clear and easing respiratory conditions like chronic bronchitis, asthma, and COPD. It also increases the production of surfactant in the lungs. |
| Enzyme Assay |
The activity of bromhexine HCl can be assessed using enzyme assays to measure its inhibition of TMPRSS2. The protease is incubated with its substrate in the presence of varying concentrations of bromhexine HCl. The inhibition of substrate cleavage is measured. The IC50 for TMPRSS2 inhibition is determined from dose-response curves.
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| Cell Assay |
To evaluate the cellular effects of bromhexine HCl, respiratory epithelial cells are treated with the compound, and the effects on mucus production and clearance are assessed. The inhibition of TMPRSS2-mediated viral entry can be evaluated in SARS-CoV-2 infection models. Autophagy activation is assessed by measuring LC3-II accumulation.
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| Animal Protocol |
In vivo studies with bromhexine HCl typically involve administration to animals or humans via oral routes. In models of respiratory diseases, the compound's effects on mucus clearance, inflammation, and lung function are assessed. In SARS-CoV-2 infection models, its effects on viral load and disease progression are evaluated.
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| ADME/Pharmacokinetics |
Bromhexine HCl has a molecular formula of C14H20Br2N2·HCl and a molecular weight of 412.59. Its CAS number is 611-75-6. The compound is a mucolytic agent. It is soluble in water and organic solvents. The purity is typically >98%.
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| Toxicity/Toxicokinetics |
Bromhexine HCl is generally well-tolerated. Common side effects may include gastrointestinal disturbances. As with all drugs, it should be used under medical supervision. Specific toxicity data are not detailed in the available literature.
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| References |
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| Additional Infomation |
Bromhexine hydrochloride is the hydrochloride salt formed by the reaction of equimolar amounts of bromhexine and hydrogen chloride. It is used as an expectorant to treat respiratory diseases accompanied by expectoration of sputum. It has expectorant properties and contains bromhexine (1+) ions. Bromhexine hydrochloride is the hydrochloride form of bromhexine (a secretion inhibitor with expectorant activity). After administration, bromhexine enhances lysosomal activity, promoting the hydrolysis of acidic mucopolysaccharide polymers in the respiratory tract. This increases the production of serous mucus in the respiratory tract, thinning the sputum and reducing its viscosity. This helps it exert its secretory effect, making it easier for cilia to expel sputum from the lungs. It clears respiratory mucus and helps treat respiratory diseases associated with abnormal thick mucus, excessive mucus secretion, and impaired mucus transport. A mucolytic agent used to treat respiratory diseases associated with thick or excessive mucus. (Excerpt from Martindale Pharmacopoeia, 30th edition, p. 744) See also: Bromhexine (containing the active ingredient).
Bromhexine HCl is a mucolytic agent used for respiratory conditions associated with increased mucus secretion. It is also a potent TMPRSS2 protease inhibitor that can prevent and manage SARS-CoV-2 infection. It is an autophagy activator. |
| Molecular Formula |
C14H21BR2CLN2
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| Molecular Weight |
412.5909
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| Exact Mass |
409.975
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| CAS # |
611-75-6
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| Related CAS # |
Bromhexine-d3 hydrochloride
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| PubChem CID |
5702220
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| Appearance |
White to off-white solid powder
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| Boiling Point |
441.5ºC at 760 mmHg
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| Melting Point |
240-244 °C
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| Flash Point |
220.8ºC
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| LogP |
5.941
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
256
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UCDKONUHZNTQPY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H20Br2N2.ClH/c1-18(12-5-3-2-4-6-12)9-10-7-11(15)8-13(16)14(10)17;/h7-8,12H,2-6,9,17H2,1H3;1H
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| Chemical Name |
2,4-dibromo-6-[[cyclohexyl(methyl)amino]methyl]aniline;hydrochloride
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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. |
| 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) |
DMSO : ~20 mg/mL (~48.47 mM)
H2O : ~3.33 mg/mL (~8.07 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (4.85 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 20.0 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. Solubility in Formulation 2: ≥ 2 mg/mL (4.85 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 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2.22 mg/mL (5.38 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4237 mL | 12.1186 mL | 24.2371 mL | |
| 5 mM | 0.4847 mL | 2.4237 mL | 4.8474 mL | |
| 10 mM | 0.2424 mL | 1.2119 mL | 2.4237 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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