Ambroxol HCl

Catalog No.S3064

For research use only.

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.

Ambroxol HCl Chemical Structure

CAS No. 23828-92-4

Purity & Quality Control

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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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 414.56
Formula

C13H18Br2N2O.HCl

CAS No. 23828-92-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(CCC1NCC2=C(C(=CC(=C2)Br)Br)N)O.Cl

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05287503 Recruiting Drug: Ambroxol Hydrochloride|Drug: Placebo Parkinson Disease|GBA Gene Mutation Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta|IRCCS National Neurological Institute C. Mondino Foundation|University of Campania Luigi Vanvitelli February 15 2022 Phase 2
NCT04405596 Not yet recruiting Drug: Ambroxol Hydrochloride|Other: Placebo Lewy Body Disease Lawson Health Research Institute September 2020 Phase 1|Phase 2
NCT04388969 Recruiting -- Gaucher Disease|Parkinson Disease|GBA Gene Mutation Shaare Zedek Medical Center May 6 2020 --
NCT02941822 Completed Drug: Ambroxol Parkinson Disease University College London|The Cure Parkinson''s Trust December 2016 Phase 2
NCT02914366 Unknown status Drug: Ambroxol|Other: Placebo Parkinson''s Disease Dementia Lawson Health Research Institute|Weston Brain Institute|University of Western Ontario Canada|London Health Sciences Centre November 2015 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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