Ambroxol HCl

Catalog No.S3064

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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Ambroxol HCl Chemical Structure

Ambroxol HCl Chemical Structure
Molecular Weight: 414.56

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Quality Control & MSDS

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Ambroxol HCl is available in the following compound libraries:

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Product Description

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]
IC50 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.
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Electrophysiology. Na+ currents are recorded in the whole-cell, voltage-clamp configuration at room temperature. The extracellular solution contains 140.0 mM NaCl, 5.3 mM KCl, 27.0 mM glucose, 10.0 mM HEPES, 0.8 mM MgCl2, and 1.8 mM CaCl2, pH 7.4. In most of the experiments on DRG neurons, 300 nM tetrodotoxin (TTX) is added. The intracellular medium consists of 50.0 mM CsCl, 90.0 mM CsF, 10.0 mM NaF, 10.0 mM HEPES, 10.0 mM EGTA, and 2.0 mM MgCl2, pH 7.4. Recording pipettes have resistances of 0.8 to 1.8 MΩ when filled with intracellular solution. Currents are recorded using an EPC-9 amplifier.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Weiser T, et al. Mol Pharmacol, 2002, 62(3), 433-438.

[2] Gibbs BF, et al. Inflamm Res, 1999, 48(2), 86-93.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-06-27)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
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
NCT01713179 Completed In the Present Study, we Investigated the Effects of Oral Ambroxol on Tear Film and Ocular Surface. Hallym University Medical Center August 2011 Phase 1|Phase 2
NCT01361802 Completed Pharyngitis|Pain Boehringer Ingelheim May 2011 Phase 2
NCT02194283 Completed Healthy Boehringer Ingelheim October 2009 Phase 1

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Chemical Information

Download Ambroxol HCl SDF
Molecular Weight (MW) 414.56
Formula

C13H18Br2N2O.HCl

CAS No. 23828-92-4
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 3 mg/mL (7.23 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <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 Name Cyclohexanol, 4-[[(2-amino-3,5-dibromophenyl)methyl]amino]-, hydrochloride (1:1), trans-

Tech Support & FAQs

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