Chlorpheniramine Maleate

Alias: NCI-C55265; Piriton; Chlortrimeton; Deconamine; Neorestamin; NCIC55265; NCI C55265; Chlo-Amine; Chlor-100; Chlor-Trimeton
Cat No.:V1240 Purity: ≥98%
Chlorpheniramine Maleate (Piriton; Chlortrimeton; Deconamine; Neorestamin; NCIC-55265; NCIC55265; Chlo-Amine; Chlor-100; Chlor-Trimeton), the Maleate salt of Chlorpheniramine, is a potent and 1st-generation alkylamine-based histamine H1 receptor antagonist with anti-allergic effects.
Chlorpheniramine Maleate Chemical Structure CAS No.: 113-92-8
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
2g
5g
10g
25g
Other Sizes

Other Forms of Chlorpheniramine Maleate:

  • Chlorpheniramine
  • Chlorpheniramine-d4 maleate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Chlorpheniramine Maleate (Piriton; Chlortrimeton; Deconamine; Neorestamin; NCIC-55265; NCIC55265; Chlo-Amine; Chlor-100; Chlor-Trimeton), the Maleate salt of Chlorpheniramine, is a potent and 1st-generation alkylamine-based histamine H1 receptor antagonist with anti-allergic effects. It suppresses the histamine H1 receptor with an IC50 of 12 nM. Chlorpheniramine has been extensively employed in the management and avoidance of allergic reaction symptoms, including urticaria and rhinitis.

Biological Activity I Assay Protocols (From Reference)
Targets
H1 Receptor ( IC50 = 12 nM )
ln Vitro

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

ln Vivo
Oral Chlorpheniramine administration prevents histamine-induced death in guinea pigs with an ED50 of 0.17 mg/kg.[1] Compared to long-duration scratching observed in NC/Nga mice, 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 in other mice. [6] The administration of 20 mg/kg of chlorpheniramine significantly reduces the increase in REM sleep that immobilization stress causes in rats. This is because the histaminergic and cholinergic mechanisms that produce REM sleep are blocked.[7]
Enzyme Assay
Segments of isolated ileum, measuring 1 centimeter, are suspended in an organ bath that contains Tyrode solution at 32 degrees Celsius (ventilation). Using an isotonic transducer, the contractile reactions to histamine (0.54 μM) are measured. Five minutes prior to the addition of histamine, an organ bath is filled with a predetermined concentration of chlorpheniramine. The probit method is used to determine the IC50 value of chlorpheniramine.
Cell Assay
For 48 hours, cells are exposed to different chlorpheniramine concentrations. To assess cell growth, cells are cleaned, separated, and counted using a Coulter counter.
Animal Protocol
Suspended in 1% (v/v) Tween 80; 10 mg/kg; ral gavage
Male NC/Nga mice, male ICR mice and female BALB/c mice with atopic dermatitis
References

[1]. J Med Chem . 1986 Jul;29(7):1178-83.

[2]. J Med Chem . 1991 Apr;34(4):1314-28.

[3]. Breast Cancer Res Treat . 1995 Aug;35(2):187-94.

[4]. Antimicrob Agents Chemother . 2007 Nov;51(11):4133-40.

[5]. J Pharmacol Exp Ther . 2009 Aug;330(2):403-12.

[6]. Eur J Pharmacol . 2003 Jun 27;471(3):223-8.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H23CLN2O4
Molecular Weight
390.86
Exact Mass
390.13
Elemental Analysis
C, 61.46; H, 5.93; Cl, 9.07; N, 7.17; O, 16.37
CAS #
113-92-8
Related CAS #
Chlorpheniramine; 132-22-9; Chlorpheniramine-d4 maleate; 2747915-71-3
Appearance
White crystalline solid
SMILES
CN(C)CCC(C1=CC=C(C=C1)Cl)C2=CC=CC=N2.C(=C\C(=O)O)\C(=O)O
InChi Key
DBAKFASWICGISY-BTJKTKAUSA-N
InChi Code
InChI=1S/C16H19ClN2.C4H4O4/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13;5-3(6)1-2-4(7)8/h3-9,11,15H,10,12H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
Chemical Name
(Z)-but-2-enedioic acid;3-(4-chlorophenyl)-N,N-dimethyl-3-pyridin-2-ylpropan-1-amine
Synonyms
NCI-C55265; Piriton; Chlortrimeton; Deconamine; Neorestamin; NCIC55265; NCI C55265; Chlo-Amine; Chlor-100; Chlor-Trimeton
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~78 mg/mL (~199.6 mM)
Water: ~78 mg/mL (~199.6 mM)
Ethanol: ~78 mg/mL (~199.6 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: Saline: 20 mg/mL

Solubility in Formulation 5: 120 mg/mL (307.02 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5585 mL 12.7923 mL 25.5846 mL
5 mM 0.5117 mL 2.5585 mL 5.1169 mL
10 mM 0.2558 mL 1.2792 mL 2.5585 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05520944 Active
Recruiting
Drug: ClorNovir® (Chlorpheniramine)
0.4% Nasal Spray
COVID-19
COVID-19 Pandemic
SARS CoV 2 Infection
Dr. Ferrer BioPharma August 26, 2021 N/A
NCT04688736 Recruiting Drug: Placebo
Drug: Chlorpheniramine
Allergic Transfusion Reaction Institute of Hematology & Blood
Diseases Hospital, China
January 1, 2021 Phase 2
NCT05858216 Not yet recruiting Drug: Chlor-Trimeton Voice Disorder Due to Iatrogenic
Factor
Auburn University May 15, 2023 Early Phase 1
NCT00837837 Completed Drug: Chlorpheniramine Allergic Reactions Wyeth is now a wholly owned
subsidiary of Pfizer
December 21, 2008 Phase 1
NCT02246166 Completed Drug: Test tablet
Other: Placebo
Common Cold GlaxoSmithKline January 2015 Phase 4
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