In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
Saline
Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.
20.000mg/ml
(51.17mM)
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.)
Preparing Stock Solutions
Biological Activity
Description
Chlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is an Histamine H1 receptor antagonist with an IC50 of 12 nM.
Targets
Histamine H1 receptor
12 nM
In vitro
Chlorpheniramine inhibits [3H]mepyramine binding to the Histamine H1 receptor in guinea pig cortex with an IC50 of 8.8 nM. Chlorpheniramine inhibits the proliferation of MCF-7, MDA-MB 231, and Ehrlich cells in a dose-response manner, and significantly reduces ornithine decarboxylase mRNA translation by 50%-70% at 250 μM. Chlorpheniramine displaces [3H]pyrilamine from human Histamine Receptor subtype 1 expressed in CHO cells with an IC50 of 66 nM. Chlorpheniramine displays antimalarial activity against CQS strain (D6) and MDR strain (Dd2) of P. falciparum with IC50s of 61.2 uM and 3.9 uM, respectively. Chlorpheniramine displays cytotoxicity against the proliferation of concanavalin A-induced murine splenic lymphocytes with an IC50 of 33.4 μM. Chlorpheniramine treatment in human salivary gland cells more significantly inhibits the histamine-induced [Ca2+]i increase in a concentration-dependent manner with an IC50 of 128 nM than that of carbachol-induced [Ca2+]i increase with an IC50 of 43.9 μM.
In Vivo
Oral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg. 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. 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.
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 to the organ bath 5 minutes before the addition of histamine. The IC50 value of Chlorpheniramine is calculated by the probit 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.
RETURN POLICY
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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.