1. Anti-infection Autophagy
  2. SARS-CoV Autophagy HIV
  3. Bromhexine hydrochloride

Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions.

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Bromhexine hydrochloride Chemical Structure

Bromhexine hydrochloride Chemical Structure

CAS No. : 611-75-6

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Based on 3 publication(s) in Google Scholar

Other Forms of Bromhexine hydrochloride:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions[1][2][3][4].

IC50 & Target[4]

HIV-1

 

In Vitro

Bromhexine hydrochloride (BHH; 250μM; 24 hours) also significantly attenuates HGF-induced invasion of LNCaP and C4-2B cells that natively express TMPRSS2[1].
No significant toxicity is observed over a 48-hour period exposing LNCaP, DU145, PC3, or HepG2 cells to Bromhexine hydrochloride concentrations ranging from 0μM to 250μM. Bromhexine hydrochloride exposure does not induce cell death or substantially suppress the growth of DU145 cells[1].
Bromhexine hydrochloride (20?μM; 48?h) inhibits dendritic cells infection with HIV-1[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bromhexine hydrochloride (30mg/kg; ip; three times per week for 5 weeks) significantly reduces the incidence of distant metastasis to lung and liver sites from 55% in vehicle-treated animals to 20% in Wild-type C57BL/6 and TRAMP mice with PIN (prostatic intraepithelial neoplasia). The prostate glands of the mice treated with Bromhexine hydrochloride are generally substantially larger than vehicle-treated TRAMP mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

412.59

Formula

C14H21Br2ClN2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(C1CCCCC1)CC2=CC(Br)=CC(Br)=C2N.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (48.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 3.33 mg/mL (8.07 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (4.85 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (4.85 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 2.22 mg/mL (5.38 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.4237 mL 12.1186 mL 24.2371 mL 60.5928 mL
5 mM 0.4847 mL 2.4237 mL 4.8474 mL 12.1186 mL
DMSO 10 mM 0.2424 mL 1.2119 mL 2.4237 mL 6.0593 mL
15 mM 0.1616 mL 0.8079 mL 1.6158 mL 4.0395 mL
20 mM 0.1212 mL 0.6059 mL 1.2119 mL 3.0296 mL
25 mM 0.0969 mL 0.4847 mL 0.9695 mL 2.4237 mL
30 mM 0.0808 mL 0.4040 mL 0.8079 mL 2.0198 mL
40 mM 0.0606 mL 0.3030 mL 0.6059 mL 1.5148 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Bromhexine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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