| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Ambroxol targets multiple pathways involved in mucus clearance and inflammation. It acts on the mucous membranes to restore physiologic clearance mechanisms of the airways. Ambroxol dissolves mucus, stimulates mucus production, and stimulates the synthesis and release of surfactant by type II pneumocytes. It is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol also induces lung autophagy.
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| ln Vitro |
In vitro, Ambroxol has been shown to exert several activities, including secretolytic activity, anti-inflammatory activity, and antioxidant activity. It promotes mucus clearance, facilitates expectoration, and eases productive cough. Ambroxol has been shown to increase glucocerebrosidase activity and to induce autophagy in lung cells. The compound has also been shown to have anti-inflammatory and antioxidant effects.
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| ln Vivo |
Ambroxol (NA-872; 1, 3, 4, 5 mM in drinking water for 12 days) causes disease in transgenic mice expressing the heterozygous L444P mutation in the murine glucocerebrosidase 1 gene, and in mice overexpressing human α-synuclein [2].
In vivo, Ambroxol has been shown to be effective in the treatment of bronchopulmonary diseases with abnormal mucus secretion and transport. Clinical studies have demonstrated its efficacy in reducing sputum viscosity and improving expectoration in patients with chronic bronchitis, COPD, and other respiratory diseases. Ambroxol has also been studied for its potential in Parkinson disease and Gaucher disease. |
| Enzyme Assay |
In vitro enzyme assays for Ambroxol typically involve measuring its effect on glucocerebrosidase (GCase) activity. The enzyme is incubated with its substrate in the presence of varying concentrations of Ambroxol, and the production of the product is measured. The EC50 for enhancement of GCase activity is determined. The compound's effect on autophagy can be assessed by measuring the levels of autophagy markers such as LC3-II in cultured cells.
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| Cell Assay |
In vitro cell-based studies with Ambroxol typically involve cultured lung epithelial cells, macrophages, or neurons. Cells are treated with Ambroxol at various concentrations. Mucus production and secretion are measured. The effect of Ambroxol on surfactant production by type II pneumocytes is assessed. The compound's anti-inflammatory and antioxidant effects are evaluated by measuring cytokine production and oxidative stress markers. Autophagy is assessed by measuring LC3-II levels.
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| Animal Protocol |
In vivo animal studies with Ambroxol are typically conducted in rodent models of respiratory diseases. The compound is administered orally or intraperitoneally. The effect of Ambroxol on sputum viscosity, mucus clearance, and cough is assessed. The compound's efficacy in reducing inflammation and oxidative stress in the lungs is evaluated. Pharmacokinetic studies are performed to evaluate the absorption, distribution, and elimination of the compound.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Known human metabolites of ambroxol include 4-aminocyclohexanol, cis- and 2-amino-3,5-dibromobenzaldehyde. Ambroxol is a well-characterized drug with established pharmacokinetic properties. Following oral administration, it is rapidly absorbed from the gastrointestinal tract. Ambroxol has a bioavailability of approximately 70-80%. It is extensively metabolized in the liver to various metabolites. The elimination half-life is approximately 7-12 hours. Ambroxol is excreted in the urine primarily as metabolites. |
| Toxicity/Toxicokinetics |
Ambroxol is a clinically approved drug with a well-established safety profile. The most common adverse effects are mild and include gastrointestinal upset, nausea, and vomiting. Allergic reactions, including skin rash and urticaria, can occur. Ambroxol is generally well-tolerated at therapeutic doses. The compound is available over-the-counter in many countries.
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| References |
[1]. Vojo Deretic, et al. Enhancement of lung levels of antibiotics by ambroxol and bromhexine. Expert Opin Drug Metab Toxicol. 2019 Mar;15(3):213-218.
[2]. Anna Migdalska-Richards, et al. Ambroxol effects in glucocerebrosidase and α-synuclein transgenic mice. Ann Neurol. 2016 Nov;80(5):766-775. |
| Additional Infomation |
Ambroxol is an aromatic amine. It has been reported and data is available for its discovery in Justicia adhatoda. It is a metabolite of bromhexine, which stimulates mucociliary movement and clears airways from the respiratory tract. It is usually administered as a hydrochloride salt. See also: Ambroxol (note moved to).
Ambroxol is a clinically approved mucoactive agent used for the treatment of respiratory diseases associated with viscid mucus. It is available in various formulations, including tablets, syrups, and inhalation solutions. Ambroxol is marketed under various brand names, including Mucosolvan. It is also being investigated for its potential therapeutic applications in Parkinson disease and Gaucher disease. |
| Molecular Formula |
C13H18N2OBR2
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|---|---|
| Molecular Weight |
378.10282
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| Exact Mass |
375.978
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| CAS # |
18683-91-5
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| Related CAS # |
Ambroxol hydrochloride;23828-92-4
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| PubChem CID |
2132
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
468.6±45.0 °C at 760 mmHg
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| Melting Point |
233-234ºC
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| Flash Point |
237.2±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.654
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| LogP |
2.91
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
259
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O[C@H]1CC[C@H](NCC2=CC(Br)=CC(Br)=C2N)CC1
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| InChi Key |
JBDGDEWWOUBZPM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H18Br2N2O/c14-9-5-8(13(16)12(15)6-9)7-17-10-1-3-11(18)4-2-10/h5-6,10-11,17-18H,1-4,7,16H2
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| Chemical Name |
4-[(2-amino-3,5-dibromophenyl)methylamino]cyclohexan-1-ol
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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 |
| 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 : ≥ 200 mg/mL (~528.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (13.22 mM) in 5% DMSO + 95% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (6.61 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.61 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. Solubility in Formulation 4: ≥ 2.5 mg/mL (6.61 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 corn oil and mix evenly. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6448 mL | 13.2240 mL | 26.4480 mL | |
| 5 mM | 0.5290 mL | 2.6448 mL | 5.2896 mL | |
| 10 mM | 0.2645 mL | 1.3224 mL | 2.6448 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06614894 | Not yet recruiting | Drug: Ambroxol Hydrochloride 30 mg tablet - 9 mg/kg/day Drug: Ambroxol Hydrochloride 30 mg tablet - 18 mg/kg/day Drug: Ambroxol Hydrochloride 30 mg tablet - 27 mg/kg/day |
MPS3 Sanfilippo Syndrome |
Ozlem Goker-Alpan | 2024-12-01 | Phase 2 Phase 3 |
| NCT02036775 | Completed | Drug: Lasolvan tablet Drug: Lasolvan tablet Drug: Lasolvan tablet |
Healthy | Boehringer Ingelheim | 2014-03 | Phase 1 |
| NCT05778617 | Not yet recruiting | Drug: Ambroxol Hydrochloride (420mg) Drug: Placebo |
Parkinson Disease | University College, London | 2024-10 | Phase 3 |
| NCT05287503 | Active, not recruiting | Drug: Ambroxol Hydrochloride Drug: Placebo |
GBA Gene Mutation Parkinson Disease |
Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta | 2022-02-15 | Phase 2 |
| NCT02941822 | Completed | Drug: Ambroxol | Parkinson Disease | University College, London | 2016-12 | Phase 2 |
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