Cat. No.: HY-B0286

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Chlorpheniramine

(Synonyms: Chlorphenamine)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research.

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

Purity: 99.86%
CAS No.: 132-22-9
Formula: C₁₆H₁₉ClN₂
Molecular Weight:274.79

Storage:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Chlorpheniramine Chemical Structure

CAS No.: 132-22-9

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research^[1]^[2].

IC₅₀ & Target

IC50: 43μM in BV2 microglial cells

All Histamine Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.066 μM Compound: Chlorpheniramine	Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells Displacement of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells	[PMID: 17846138]
MDCK	IC₅₀	14 μM Compound: Chlorpheniramine	TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT1-expressing MDCK cells	[PMID: 11758759]
MDCK	IC₅₀	26 μM Compound: Chlorpheniramine	TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells TP_TRANSPORTER: inhibition of TEA uptake (TEA: 50 uM) in OCT2-expressing MDCK cells	[PMID: 11758759]
RBL-2H3	IC₅₀	0.0318 μM Compound: Chlorpheniramine	Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced mast cell degranulation preincubated with compound for 30 mins and then treated with C48/80 for 1 hr by neutral red dye based method	[PMID: 31703894]
RBL-2H3	IC₅₀	0.0536 μM Compound: Chlorpheniramine	Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced histamine release preincubated with compound for 30 mins followed by C48/80 stimulation for 1 hr Antiallergic activity in rat RBL2H3 cells assessed as inhibition of C48/80-induced histamine release preincubated with compound for 30 mins followed by C48/80 stimulation for 1 hr	[PMID: 31703894]
RBL-2H3	IC₅₀	0.121 μM Compound: Chlorpheniramine	Antiallergic activity in IgE/Ag-stimulated rat RBL2H3 cells assessed as inhibition of HSA-induced beta-hexosaminidase release preincubated with compound for 30 mins and then stimulated with HSA for 15 mins followed by incubation with P-nitrophenyl-N-acety Antiallergic activity in IgE/Ag-stimulated rat RBL2H3 cells assessed as inhibition of HSA-induced beta-hexosaminidase release preincubated with compound for 30 mins and then stimulated with HSA for 15 mins followed by incubation with P-nitrophenyl-N-acety	[PMID: 31703894]
Splenocyte	IC₅₀	33.4 μM Compound: Chlorpheniramine	Cytotoxicity against C57BL/6J mouse splenocytes after 72 hrs by alamar blue assay Cytotoxicity against C57BL/6J mouse splenocytes after 72 hrs by alamar blue assay	[PMID: 17846138]

In Vitro

Chlorpheniramine shows antimalarial activity against P. falciparum (IC₅₀: 61.2 and 3.9 μM for D6 and Dd2 strain)^[4].
Chlorpheniramine reduces the proton currents (IC₅₀: 43 μM) in BV2 microglial cells^[1].

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

Cell Viability Assay

Cell Line:

Murine microglial BV2 cells^[1].
Concentration:

100 μM
Incubation Time:

5 min
Result:

Inhibited proton currents with moderate potency.

In Vivo

Chloropheniramine (50, 100 and 200 μg/kg; IM; 3 times, at intervals of 1 week) enhances white blood cells in the peripheral blood^[2].
Chlorpheniramine (10 mg/kg, p.o) inhibits scratching in Ovalbumin (HY-W250978)-challenged BALB/c mice^[3].

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

Animal Model:

Sprague-Dawley (SD) rats^[2].
Dosage:

50, 100 and 200 μg/kg
Administration:

Chlorpheniramine (50, 100 and 200 μg/kg; IM; 3 times, at intervals of 1 week)
Result:

Enhanced white blood cells in the peripheral blood, mostly due to the increases of B cells and monocytes, but not T cells and NK cells.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 132-22-9
Appearance Liquid (Density: 1.108±0.06 g/cm³)
Molecular Weight 274.79
Formula C₁₆H₁₉ClN₂
Color Colorless to light yellow
SMILES

CN(C)CCC(C1=CC=C(Cl)C=C1)C2=CC=CC=N2
Synonyms

Chlorphenamine
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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Journal Impact Factor

Neuropharmacology

Imperatorin activates TRPV1/GRPR pathway to induce scratching behaviors in mice. [Abstract]

2025 Nov 1:278:110593. PMID: 40683349
J Inflamm Res

Neural-Inflammation Mechanism of Spinal Palmitic Acid Promoting Atopic Dermatitis in Mice. [Abstract]

2025 Jun 17:18:7907-7919. PMID: 40546406
J Pharm Sci

Effects of Processing on a Sustained Release Formulation Prepared by Twin-Screw Dry Granulation. [Abstract]

2019 Sep;108(9):2895-2904. PMID: 30965041
Chemosphere

Mass-balance-model-based evaluation of sewage treatment plant contribution to residual pharmaceuticals in environmental waters. [Abstract]

2019 Jun:225:378-387. PMID: 30884299

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (727.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

3.6391 mL

18.1957 mL

36.3914 mL

5 mM

0.7278 mL

3.6391 mL

7.2783 mL

10 mM

0.3639 mL

1.8196 mL

3.6391 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 5 mg/mL (18.20 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (18.20 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (18.20 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 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]. Jiwon Kim, etal. Inhibitory effects of antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells. Eur J Pharmacol. 2017 Mar 5;798:122-128. [Content Brief]

[2]. Kyung-Jin Jung, etal. Enhancement of B cell and monocyte populations in rats exposed to chlorpheniramine. Arch Pharm Res. 2012 Dec;35(12):2183-9. [Content Brief]

[3]. Takano, N., I. Arai, and M. Kurachi, Analysis of the spontaneous scratching behavior by NC/Nga mice: a possible approach to evaluate antipruritics for subjects with atopic dermatitis. Eur J Pharmacol, 2003. 471(3): p. 223-8. [Content Brief]

[4]. Kelly, J.X., et al., Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. Antimicrob Agents Chemother, 2007. 51(11): p. 4133-40. [Content Brief]

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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.6391 mL	18.1957 mL	36.3914 mL	90.9786 mL
	5 mM	0.7278 mL	3.6391 mL	7.2783 mL	18.1957 mL
	10 mM	0.3639 mL	1.8196 mL	3.6391 mL	9.0979 mL
	15 mM	0.2426 mL	1.2130 mL	2.4261 mL	6.0652 mL
	20 mM	0.1820 mL	0.9098 mL	1.8196 mL	4.5489 mL
	25 mM	0.1456 mL	0.7278 mL	1.4557 mL	3.6391 mL
	30 mM	0.1213 mL	0.6065 mL	1.2130 mL	3.0326 mL
	40 mM	0.0910 mL	0.4549 mL	0.9098 mL	2.2745 mL
	50 mM	0.0728 mL	0.3639 mL	0.7278 mL	1.8196 mL
	60 mM	0.0607 mL	0.3033 mL	0.6065 mL	1.5163 mL
	80 mM	0.0455 mL	0.2274 mL	0.4549 mL	1.1372 mL
	100 mM	0.0364 mL	0.1820 mL	0.3639 mL	0.9098 mL

Keywords

Chlorpheniramine

4 Cited Publications

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Chlorpheniramine

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Publications Citing Use of MedChemExpress (MCE) Chlorpheniramine

All Histamine Receptor Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Chlorpheniramine Related Classifications

HY-B0286 Related Classifications