Ambroxol HCl

Catalog No.S3064

Ambroxol HCl Chemical Structure

Molecular Weight(MW): 414.56

AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.
Targets
Sodium channel [1]
35.2 μM-22.5 μM
In vitro

Ambroxol inhibits Na+ channels in sensory neurons. The potency for tonic block of TTX-r channels is relatively high. Ambroxol affects the Na+ current kinetics of TTX-r and TTX-s channels differently. In CNaIIA cells, the compound behaves like a charged local anesthetic: the block is dependent on stimulus number and increases with higher frequencies in a train of depolarizing stimuli. In CNaIIA cells, ambroxol inhibits inactivated channels 5.5-fold more potently than resting channels. The corresponding factor for TTX-r channels is only 3.3.[1] Ambroxol inhibits the release of histamine, leukotrienes and cytokines from human leukocytes and mast cells. [2]

In vivo Ambroxol inhibited histamine release by more than 50% from human adenoidal mast cells (1000 microM ambroxol) and skin mast cells (100 microM ambroxol) stimulated by Con A and compound 48/80, respectively. Ambroxol (100 microM) strikingly inhibited anti-IgE induced release of both histamine, LTC4, IL-4 and IL-13 from basophils and reduced both histamine and LTB4 release induced by C5a or Zymosan in monocytes. The drug also reduced LTB4 and superoxide anion production in granulocytes stimulated by zymosan or fMLP.

Protocol

Solubility (25°C)

In vitro DMSO 4 mg/mL warmed (9.64 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 414.56
Formula

C13H18Br2N2O.HCl

CAS No. 23828-92-4
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02941822 Not yet recruiting Parkinson Disease University College, London|Cure Parkinsons Trust|PRO.MED.CS Praha a.s - Czech Republic December 2016 Phase 2
NCT02914366 Recruiting Parkinsons Disease Dementia Lawson Health Research Institute|Weston Foundation|University of Western Ontario, Canada|London Health Sciences Centre November 2015 Phase 2
NCT01463215 Suspended Type I Gaucher Disease Exsar Corporation December 2012 Phase 1|Phase 2
NCT01573663 Completed Healthy Hanmi Pharmaceutical Company Limited February 2012 Phase 1
NCT02572609 Completed Healthy Boehringer Ingelheim November 2011 Phase 1
NCT01713179 Completed In the Present Study, we Investigated the Effects of Oral Ambroxol on Tear Film and Ocular Surface. Hallym University Kangnam Sacred Heart Hospital August 2011 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID