Chlorpheniramine Maleate

Catalog No.S1816 Batch:S181601

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Technical Data

Formula

C16H19ClN2.C4H4O4
Molecular Weight 390.86 CAS No. 113-92-8
Solubility (25°C)* In vitro DMSO 78 mg/mL (199.55 mM)
Water 78 mg/mL (199.55 mM)
Ethanol 78 mg/mL (199.55 mM)
In vivo (Add solvents to the product individually and in order)
Clear solution
Saline
20.0mg/ml Taking the 1 mL working solution as an example, add 20 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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.
Targets
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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 Assay:[3]
  • 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.
Animal Study:[6]
  • Animal Models

    Male NC/Nga mice, male ICR mice and female BALB/c mice with atopic dermatitis

  • Dosages

    10 mg/kg

  • Administration

    Orally

Selleck's Chlorpheniramine Maleate has been cited by 1 publication

Histamine Receptor Antagonists, Loratadine and Azelastine, Sensitize P-gp-overexpressing Antimitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms. [ Anticancer Res, 2019, 39(7):3767-3775] PubMed: 31262903

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.