Cat. No.: HY-B0480

Brompheniramine maleate

(Synonyms: (±)-Brompheniramine maleate)

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

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 K_d 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.

For research use only. We do not sell to patients.

Purity: 99.93%
CAS No.: 980-71-2
Formula: C₂₀H₂₃BrN₂O₄
Molecular Weight:435.31

Storage:

4°C, sealed storage, away from moisture

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

Brompheniramine maleate Chemical Structure

CAS No.: 980-71-2

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[2]

H₁ Receptor

6.06 nM (Kd)

All Histamine Receptor Isoforms :

All mAChR Isoforms :

All Sodium Channel Isoforms :

All Calcium Channel Isoforms :

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 980-71-2
Appearance Solid
Molecular Weight 435.31
Formula C₂₀H₂₃BrN₂O₄
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
Synonyms

(±)-Brompheniramine maleate
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)

Publications (2)

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Journal Impact Factor

Biomaterials

Cellhesion VP enhances the immunomodulating potential of human mesenchymal stem cell-derived extracellular vesicles. [Abstract]

2021 Apr:271:120742. PMID: 33706111
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2972 mL

11.4861 mL

22.9721 mL

5 mM

0.4594 mL

2.2972 mL

4.5944 mL

10 mM

0.2297 mL

1.1486 mL

2.2972 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Chong-Chi Chiu, et al. Subcutaneous brompheniramine for cutaneous analgesia in rats. Eur J Pharmacol. 2019 Oct 5;860:172544. [Content Brief]

[2]. B Cusack, et al. Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65. [Content Brief]

[3]. Shin WH, Kim KS, Kim EJ. Electrophysiological effects of brompheniramine on cardiac ion channels and action potential. Pharmacol Res. 2006 Dec;54(6):414-20. [Content Brief]

[4]. Yasuda SU, Yasuda RP. Affinities of brompheniramine, chlorpheniramine, and terfenadine at the five human muscarinic cholinergic receptor subtypes. Pharmacotherapy. 1999 Apr;19(4):447-51. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Brompheniramine maleate

2 Cited Publications

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Brompheniramine maleate

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Publications Citing Use of MedChemExpress (MCE) Brompheniramine maleate

All Histamine Receptor Isoforms

All mAChR Isoforms

All Sodium Channel Isoforms

All Calcium Channel Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Brompheniramine maleate Related Classifications

HY-B0480 Related Classifications