Chlorpheniramine Maleate

For research use only.

Catalog No.S1816 Synonyms: NCI-C55265

1 publication

Chlorpheniramine Maleate Chemical Structure

Molecular Weight(MW): 390.86

Chlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is an histamine H1 receptor antagonist with IC50 of 12 nM.

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10mM (1mL in DMSO) EUR 127 In stock
EUR 95 In stock
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Selleck's Chlorpheniramine Maleate has been cited by 1 publication

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Biological Activity

Description Chlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is an histamine H1 receptor antagonist with IC50 of 12 nM.
Histamine H1 receptor [1]
12 nM
In vitro

Chlorpheniramine inhibits the [3H]mepyramine binding to the histamine H1 receptor in guinea pig cortex with IC50 of 8.8 nM. [2] Chlorpheniramine inhibits the proliferation of MCF-7, MDA-MB 231, and Ehrlich cells in a dose-response manner, and significantly reduces the ornithine decarboxylase mRNA translation by 50%-70% at the 250 μM. [3] Chlorpheniramine displaces of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells with IC50 of 66 nM. Chlorpheniramine displays antimalarial activity against CQS strain (D6) and MDR strain (Dd2) of P. falciparum with IC50 of 61.2 uM and 3.9 uM, respectively. Chlorpheniramine displays cytotoxicity against the proliferation of concanavalin A-induced murine splenic lymphocytes with IC50 of 33.4 μM. [4] Chlorpheniramine treatment in human salivary gland cells more significantly inhibits the histamine-induced [Ca2+]i increase in a concentration-dependent manner with IC50 of 128 nM than that of carbachol-induced [Ca2+]i increase with an IC50 of 43.9 μM. [5]

In vivo Oral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg. [1] Oral administration of Chlorpheniramine (10 mg/kg) significantly inhibits short-duration scratching in BALB/c mice stimulated by ovalbumin active cutaneous anaphylaxis and in ICR mice subcutaneously injected with histamine, but not long-duration scratching seen in NC/Nga mice, in contrast to that of dexamethasone or tacrolimus. [6] Administration of Chlorpheniramine (20 mg/kg) significantly abolishes the increase in REM sleep in rats induced by immobilization stress due to the blockage of the histaminergic and cholinergic mechanisms generating REM sleep. [7]


Kinase Assay:[1]
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H1-Antihistaminic Activity:

The segments (1 cm) of isolated ileum from guinea pigs are suspended in an organ bath containing Tyrode solution (ventilation, 32 °C). The contractile responses to histamine (0.54 μM) are measured with an isotonic transducer. A set concentration of Chlorpheniramine is added in the organ bath 5 minutes before the addition of histamine. IC50 value of Chlorpheniramine is calculated by the probit methond.
Cell Research:[3]
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  • Cell lines: MCF-7, MDA-MB 231, and Ehrlich
  • Concentrations: Dissolved in water, final concentrations ~500 μM
  • Incubation Time: 48 hours
  • Method: Cells are exposed to various concentrations of Chlorpheniramine for 48 hours. Cells are washed, detached, and counted with a Coulter counter for the determination of cell growth.
    (Only for Reference)
Animal Research:[6]
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  • Animal Models: Male NC/Nga mice, male ICR mice and female BALB/c mice with atopic dermatitis
  • Dosages: 10 mg/kg
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.55 mM)
Water 78 mg/mL (199.55 mM)
Ethanol '78 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
20 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 390.86


CAS No. 113-92-8
Storage powder
in solvent
Synonyms NCI-C55265
Smiles CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2.C(=CC(=O)O)C(=O)O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID