| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| ln Vitro |
Pheniraminemaleate slows down metabolism and prolongs the effects of antihistamines by inhibiting CYP2D6, a particular P450 isoenzyme [1]. With an IC50 value of 1.01 mM, pheniraminemaleate suppresses histamine, which modifies cellular Ca2+ transmembrane effects and prevents Ca2+ influx into BC3H-1 cells[2]. Within 24 hours, human T-cell acute lymphoblastic leukemia cell lines treated with pheniraminemaleate (0.5, 1.0 mM) undergo apoptosis [3]. IC50s for pheniraminemaleate (1 μM-1 mM; 12-48 h) are 550 μM for CCRF-CEM cells and 420 μM for Jurkat cells, respectively, showing a time-dependent inhibition of cell growth [3].
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| ln Vivo |
In rats, pheniraminemaleate (1.75 μM) results in spinal cord block and local anesthesia [4].
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| Cell Assay |
Cell viability assay [3]
Cell Types: Human T cell acute lymphoblastic leukemia Cell Types: CCRF-CEM and Jurkat ALL Tested Concentrations: 0.5, 1.0 mM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of apoptosis, chromatin condensation and marginalization, and nuclear fragments diffuse into the cytoplasm. Cell viability assay [3] Cell Types: Human T cell acute lymphoblastic leukemia Cell Types: CCRF-CEM and Jurkat ALL Tested Concentrations: 1 μM-1 mM Incubation Duration: 12, 24, 48 hrs (hours) Experimental Results: Inhibition of cell proliferation and survival time and dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Sprague–Dawley rat (300-350 g; male) [4]
Doses: 0.30, 0.60, 0.90, 1.50, 1.75 μM Route of Administration: Intrathecal; Primary Experimental Results:Spinal block produced, and dose indicated Dependency effect. At 1.75 μM, motor function, proprioception, and nociception were 100% blocked, and the duration of action for complete recovery was approximately 41, 56, and 88 minutes, respectively. |
| References |
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| Additional Infomation |
Pheniramine maleate is a white powder with a faint amine-like odor. Melting point 107 °C. pH (1% solution) 4.5-5.5. Used medicinally as an antihistamine.
Pheniramine maleate is an organic molecular entity. Pheniramine Maleate is the maleate salt form of pheniramine, an alkylamine derivative with antihistaminic and vasodilatory properties. Pheniramine maleate binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of endothelium-derived relaxing factor, nitric oxide. Subsequent lack of activation of guanylyl cyclase through nitric oxide results in decreased cyclic GMP (cGMP) levels, thereby inhibiting constriction of smooth muscle tissue, and decreased capillary permeability and histamine-activated allergic reactions. One of the HISTAMINE H1 ANTAGONISTS with little sedative action. It is used in treatment of hay fever, rhinitis, allergic dermatoses, and pruritus. |
| Molecular Formula |
C20H24N2O4
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|---|---|
| Molecular Weight |
356.4156
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| Exact Mass |
356.173
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| CAS # |
132-20-7
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| Related CAS # |
Pheniramine;86-21-5
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| PubChem CID |
5282139
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| Appearance |
White to off-white solid powder
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| Boiling Point |
348.3ºC at 760 mmHg
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| Melting Point |
104-108°C
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| Flash Point |
164.5ºC
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| Vapour Pressure |
5.07E-05mmHg at 25°C
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| LogP |
2.877
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
340
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCC(C1=CC=CC=C1)C2=CC=CC=N2.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
SSOXZAQUVINQSA-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C16H20N2.C4H4O4/c1-18(2)13-11-15(14-8-4-3-5-9-14)16-10-6-7-12-17-16;5-3(6)1-2-4(7)8/h3-10,12,15H,11,13H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
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| Chemical Name |
(Z)-but-2-enedioic acid;N,N-dimethyl-3-phenyl-3-pyridin-2-ylpropan-1-amine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 38 mg/mL (~106.62 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8057 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.
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.
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