1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Apoptosis
  2. Histamine Receptor Apoptosis
  3. Pheniramine maleate

Pheniramine maleate  (Synonyms: Prophenpyridamine maleate; Tripoton maleate; Pheniramine maleate)

Cat. No.: HY-B0971 Purity: 99.94%
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Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects.

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

Pheniramine maleate Chemical Structure

Pheniramine maleate Chemical Structure

CAS No. : 132-20-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
USD 41 In-stock
Solution
10 mM * 1 mL in Water USD 41 In-stock
Solid
50 mg USD 38 In-stock
100 mg USD 60 In-stock
500 mg USD 96 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects[1][2][3][4].

IC50 & Target

H1 Receptor

1.01 mM (IC50)

In Vitro

Pheniramine maleate inhibits CYP2D6, the specific P450-isozymes, to delay metabolic time and prolong antihistaminic effects[1].
Pheniramine maleate regulates cellular Ca2+ transmembrane action, and inhibits Ca2+ influx into BC3H-1 cells by inhibiting histamine with an IC50 value of 1.01 mM[2].
Pheniramine maleate (0.5, 1.0 mM; 24 h) induces cell apoptosis in human T-cell acute lymphoblastic leukemia cell lines[3].
Pheniramine maleate (1 μM-1 mM; 12-48 h) inhibits cell proliferation in a time-dependent manner and shows inhibitory concentration IC50s of 550 μM (CCRF-CEM cells) and 420 μM (Jurkat cells), respectively[3].

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

Cell Viability Assay[3]

Cell Line: Human T-cell acute lymphoblastic leukemia cell lines: CCRF-CEM and Jurkat ALL
Concentration: 0.5, 1.0 mM
Incubation Time: 24 hours
Result: Induced cells apoptosis with chromatin condenses and marginalizes, and nuclear debris spreaded into the cytoplasm.

Cell Viability Assay[3]

Cell Line: Human T-cell acute lymphoblastic leukemia cell lines: CCRF-CEM and Jurkat ALL
Concentration: 1 μM-1 mM
Incubation Time: 12, 24, 48 hours
Result: Inhibited cell proliferation and survival in a time- and dose-dependent manner.
In Vivo

Pheniramine maleate (1.75 μM; i.t.) exerts local anesthesia effect and results spinal block in rats[4].

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

Animal Model: Sprague–Dawley rats (300-350 g; male)[4]
Dosage: 0.30, 0.60, 0.90, 1.50, 1.75 μM
Administration: Intrathecal injection; one time
Result: Resulted the spinal block and displayed dose-dependent effect.
Showed 100% blockades in motor function, proprioception, and nociception, with full recoveryduration of action about 41, 56, and 88 min, respectively, at 1.75 μM.
Molecular Weight

356.42

Formula

C20H24N2O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(C)CCC(C1=CC=CC=C1)C2=CC=CC=N2.O=C(O)/C=C\C(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 38 mg/mL (106.62 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8057 mL 14.0284 mL 28.0568 mL
5 mM 0.5611 mL 2.8057 mL 5.6114 mL
View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.94%

References

Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture). 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
H2O 1 mM 2.8057 mL 14.0284 mL 28.0568 mL 70.1420 mL
5 mM 0.5611 mL 2.8057 mL 5.6114 mL 14.0284 mL
10 mM 0.2806 mL 1.4028 mL 2.8057 mL 7.0142 mL
15 mM 0.1870 mL 0.9352 mL 1.8705 mL 4.6761 mL
20 mM 0.1403 mL 0.7014 mL 1.4028 mL 3.5071 mL
25 mM 0.1122 mL 0.5611 mL 1.1223 mL 2.8057 mL
30 mM 0.0935 mL 0.4676 mL 0.9352 mL 2.3381 mL
40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7535 mL
50 mM 0.0561 mL 0.2806 mL 0.5611 mL 1.4028 mL
60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1690 mL
80 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8768 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7014 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Pheniramine maleate
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