Cat. No.: HY-B1589A

Carbinoxamine maleate salt

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Carbinoxamine maleate salt is a blood-brain barrier-permeable histamine H1 receptor antagonist. Carbinoxamine maleate salt blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. Carbinoxamine maleate salt inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. Carbinoxamine maleate salt can be used in research on allergic rhinitis, influenza, etc.

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

Purity: 98.78%
CAS No.: 3505-38-2
Formula: C₂₀H₂₃ClN₂O₅
Molecular Weight:406.86

Storage:

4°C, sealed storage, away from moisture

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

Carbinoxamine maleate salt Chemical Structure

CAS No.: 3505-38-2

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

H₁ Receptor

All Histamine Receptor Isoforms :

In Vitro

Carbinoxamine maleate salt (72 h) potently inhibits infection of MDCK cells by multiple influenza A strains (H7N9, H1N1 2009, H1N1 1934, H3N2) and one influenza B strain (BY), with IC₅₀ values ranging from 3.56 to 15.54 μM^[1].
Carbinoxamine maleate salt (0-1000 μM; 72 h) exhibits low cytotoxicity against MDCK cells, with a CC₅₀ of 297.30 μM, thus showing a high selection index against various influenza virus strains^[1].
Carbinoxamine maleate salt (20 μM; 0-12 h) inhibits infection of MDCK cells by A/Shanghai/37T/2009 (H1N1) at the early stage of the viral life cycle; the inhibition rate reaches 99% when added at 0.5 h post-infection, and drops to 23% when added at 4 h post-infection^[1].
Carbinoxamine maleate salt (48 h) specifically inhibits the entry of A/Shanghai/4664T/2013 (H7N9) pseudovirus into MDCK cells, with an IC₅₀ of 8.98 μM, and does not affect the entry of other pseudoviruses or HIV-1^[1].
Carbinoxamine maleate salt (1.6-100 μM; 1.5 h) does not inhibit the neuraminidase activity of A/Puerto Rico/8/1934 (H1N1) virus even at concentrations as high as 100 μM^[1].
Carbinoxamine maleate salt (12 h) reduces viral RNA synthesis in a dose-dependent manner in MDCK cells infected with the A/Puerto Rico/8/1934 (H1N1) virus^[1].
Carbinoxamine maleate salt (10 μM; 12 h) reduces the number of NP-positive MDCK cells infected with A/Puerto Rico/8/1934 (H1N1) virus^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

Madin-Darby canine kidney (MDCK) cells
Concentration:

0, 4, 8, 16, 31, 63, 125, 250, 500, 1000 µM
Incubation Time:

72 h
Result:

Exhibited low cytotoxicity to MDCK cells with a CC₅₀ of 297.30 µM.
Resulted in selectivity index (SI = CC₅₀/IC₅₀) ranging from 19.13 (against B/Shanghai/2017(BY)) to 83.51 (against A/Shanghai/4664T/2013(H7N9)).

Immunofluorescence^[1]

Cell Line:

Madin-Darby canine kidney (MDCK) cells
Concentration:

10 µM
Incubation Time:

1 h (virus-compound co-incubation); 12 h (total culture)
Result:

Markedly reduced the number of fluorescent-staining (NP-positive) cells compared to the PBS control.

In Vivo

Carbinoxamine maleate salt (1-10 mg/kg; i.p.; daily; 5 days) provides 77.7% survival protection against lethal H7N9 influenza virus challenge in female C57BL/6 mice, while also reducing viral load and lung pathology in a dose-dependent manner^[1].

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

Animal Model:

C57BL/6 (female, 4-8 weeks old, specific-pathogen-free)^[1]
Dosage:

10 mg/kg; 1 mg/kg
Administration:

i.p.; daily; 5 days
Result:

Achieved a 77.7% survival rate at 14 days post-challenge.
Showed a survival rate higher than the PBS control (22.2%) but lower than the 10 mg/kg/day group.
Significantly reduced viral gene expression in lung tissues.
Lowered integrated optical density values of viral nucleoprotein in lung tissues.
Attenuated histopathological lung damage including reduced inflammatory cell infiltration, alveolar congestion, and alveolar wall thickening compared to the PBS control.

Chemical Information

CAS No. 3505-38-2
Appearance Solid
Molecular Weight 406.86
Formula C₂₀H₂₃ClN₂O₅
Color White to off-white
SMILES

ClC1=CC=C(C(C2=NC=CC=C2)OCCN(C)C)C=C1.O=C(O)/C=C\C(O)=O
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 (1)

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Dis Model Mech

A Drosophila chemical screen reveals targeting MEK and DGKa mitigates Ras-driven polarity-impaired tumour growth. [Abstract]

2023 Mar 1;16(3):dmm049769. PMID: 36861754

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (245.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (122.89 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

2.4578 mL

12.2892 mL

24.5785 mL

5 mM

0.4916 mL

2.4578 mL

4.9157 mL

10 mM

0.2458 mL

1.2289 mL

2.4578 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 (6.14 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 (6.14 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 (6.14 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: 100 mg/mL (245.78 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 (284 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 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]. Xu W, et al. The Antihistamine Drugs Carbinoxamine Maleate and Chlorpheniramine Maleate Exhibit Potent Antiviral Activity Against a Broad Spectrum of Influenza Viruses. Front Microbiol. 2018;9:2643. Published 2018 Nov 6. [Content Brief]

[2]. Garat BR, et al. Clinical, chemical, and pharmacologic relationships of antihistamines: A study of a new synthetic antihistaminic, carbinoxamine maleate (Clistin maleate). Journal of Allergy. 1956 Jan 1;27(1):57-62.

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
H₂O / DMSO	1 mM	2.4578 mL	12.2892 mL	24.5785 mL	61.4462 mL
	5 mM	0.4916 mL	2.4578 mL	4.9157 mL	12.2892 mL
	10 mM	0.2458 mL	1.2289 mL	2.4578 mL	6.1446 mL
	15 mM	0.1639 mL	0.8193 mL	1.6386 mL	4.0964 mL
	20 mM	0.1229 mL	0.6145 mL	1.2289 mL	3.0723 mL
	25 mM	0.0983 mL	0.4916 mL	0.9831 mL	2.4578 mL
	30 mM	0.0819 mL	0.4096 mL	0.8193 mL	2.0482 mL
	40 mM	0.0614 mL	0.3072 mL	0.6145 mL	1.5362 mL
	50 mM	0.0492 mL	0.2458 mL	0.4916 mL	1.2289 mL
	60 mM	0.0410 mL	0.2048 mL	0.4096 mL	1.0241 mL
	80 mM	0.0307 mL	0.1536 mL	0.3072 mL	0.7681 mL
	100 mM	0.0246 mL	0.1229 mL	0.2458 mL	0.6145 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

Carbinoxamine maleate salt

1 Cited Publications

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Carbinoxamine maleate salt

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Publications Citing Use of MedChemExpress (MCE) Carbinoxamine maleate salt

All Histamine Receptor Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Carbinoxamine maleate salt Related Classifications

HY-B1589A Related Classifications