2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Membrane Transporter/Ion Channel
  3. Histamine Receptor mAChR Potassium Channel Sodium Channel Calcium Channel
  4. Brompheniramine maleate

Brompheniramine maleate  (Synonyms: (±)-Brompheniramine maleate)

Cat. No.: HY-B0480 Purity: 99.78%
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Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.

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Brompheniramine maleate Chemical Structure

Brompheniramine maleate Chemical Structure

CAS No. : 980-71-2

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Based on 1 publication(s) in Google Scholar

Other Forms of Brompheniramine maleate:

Brompheniramine maleate Related Antibodies

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1 Publications Citing Use of MCE Brompheniramine maleate

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • Biological Activity

  • Purity & Documentation

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Description

Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research[1][2][3][4].

IC50 & Target[2]

H1 Receptor

6.06 nM (Kd)

In Vitro

Brompheniramine (0.1-100 μM) blocks hERG K+ channels expressed in CHO cells in a concentration-dependent manner with an IC50 of 0.90±0.14 μM, and reduced peak tail current amplitude measured at -60 mV (cells are depolarized for 2 s to +20 mV from a holding potential of -80 mV followed by a 3s repolarization back to -60 mV)[3].
Brompheniramine (1, 10 and 100 μM) significantly shortens the APD50 and depresses the plateau phase on the action potential in guinea pig papillary muscle, as well as slightly prolongs the APD90 in guinea pig papillary muscle at 10 and 100 μM[3].
Brompheniramine (0.1-100 μM) inhibit the amplitude of the Ca2+ channel currents in rat ventricular myocytes by 14.1±1.1, 31.1±5.8, 38.0±3.8 and 90.2±3.7% at 0.1, 1, 10 and 100 μM, respectively[3].
Brompheniramine blocks muscarinic cholinergic receptors in human chinese hamster ovary (CHO) cells[4].

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

Brompheniramine maleate Related Antibodies
In Vivo

Brompheniramine (0.3-3?μM; SC, single dosage) induces cutaneous analgesia in rats[1].

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

Animal Model: Male Sprague-Dawley rats[1]
Dosage: 0.3, 0.6, 1.1, 1.5 and 3.0  μM
Administration: SC, single dosage
Result: Provoked cutaneous analgesia in a dose-dependent manner, with an EC50 value of 0.66 μM, and induced prolonged analgesic duration.
Clinical Trial
Molecular Weight

435.31

Formula

C20H23BrN2O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)/C=C\C(O)=O.CN(C)CCC(C1=CC=CC=N1)C2=CC=C(Br)C=C2
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 : 100 mg/mL (229.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (229.72 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2972 mL 11.4861 mL 22.9721 mL
5 mM 0.4594 mL 2.2972 mL 4.5944 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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: 25 mg/mL (57.43 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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
DMSO / H2O 1 mM 2.2972 mL 11.4861 mL 22.9721 mL 57.4303 mL
5 mM 0.4594 mL 2.2972 mL 4.5944 mL 11.4861 mL
10 mM 0.2297 mL 1.1486 mL 2.2972 mL 5.7430 mL
15 mM 0.1531 mL 0.7657 mL 1.5315 mL 3.8287 mL
20 mM 0.1149 mL 0.5743 mL 1.1486 mL 2.8715 mL
25 mM 0.0919 mL 0.4594 mL 0.9189 mL 2.2972 mL
30 mM 0.0766 mL 0.3829 mL 0.7657 mL 1.9143 mL
40 mM 0.0574 mL 0.2872 mL 0.5743 mL 1.4358 mL
50 mM 0.0459 mL 0.2297 mL 0.4594 mL 1.1486 mL
60 mM 0.0383 mL 0.1914 mL 0.3829 mL 0.9572 mL
80 mM 0.0287 mL 0.1436 mL 0.2872 mL 0.7179 mL
100 mM 0.0230 mL 0.1149 mL 0.2297 mL 0.5743 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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Brompheniramine maleate 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.

Keywords:

Brompheniramine980-71-2(±)-BrompheniramineHistamine ReceptormAChRPotassium ChannelSodium ChannelCalcium ChannelMuscarinic acetylcholine receptorKcsANa channelsNa+ channelsCa2+ channelsCa channelsanticholinergicantidepressantsedativecommon coldallergic rhinitisantihistamineInhibitorinhibitorinhibit

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