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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].
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| 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].
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| References |
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| Additional Infomation |
Bromhexine hydrochloride is a hydrochloride resulting from the reaction of equimolar amounts of bromhexine and hydrogen chloride. It is used as a mucolytic for the treatment of respiratory disorders associated with productive cough (i.e. a cough characterised by the production of sputum). It has a role as a mucolytic. It contains a bromhexine(1+).
Bromhexine Hydrochloride is the hydrochloride salt form of bromhexine, a secretolytic, with mucolytic activity. Upon administration, bromhexine increases lysosomal activity and enhances hydrolysis of acid mucopolysaccharide polymers in the respiratory tract. This increases the production of serous mucus in the respiratory tract, which makes the phlegm thinner and decreases mucus viscosity. This contributes to its secretomotoric effect, and allows the cilia to more easily transport the phlegm out of the lungs. This clears mucus from the respiratory tract and may aid in the treatment of respiratory disorders associated with abnormal viscid mucus, excessive mucus secretion and impaired mucus transport. A mucolytic agent used in the treatment of respiratory disorders associated with viscid or excessive mucus. (From Martindale, The Extra Pharmacopoeia, 30th ed, p744) See also: Bromhexine (has active moiety). |
| 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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