| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
| Targets |
H1 Receptor; VEGFR-3
Chloropyramine hydrochloride targets the histamine H1 receptor as a potent antagonist. It also inhibits VEGFR-3 and FAK biochemical functions. The compound has anti-cholinergic and antispasmodic properties. Its mechanism involves blocking histamine-mediated allergic responses by competitively inhibiting H1 receptor activation. |
|---|---|
| ln Vitro |
Chloropyramine hydrochloride (Compound 1) treatment highly sensitively affects BT474 cells, resulting in a 40% reduction in viability at 1 µM concentrations after 48 hours. The viability of control MCF7-pcDNA3 cells is found to be significantly higher than that of MCF7-VEGFR-3 cells at 1 µM concentrations of Chloropyramine hydrochloride (P<0.01), and this difference doubles at 10 µM concentration (P<0.001). Treatment with chloropyramine hydrochloride also causes a concentration-dependent reduction in cell proliferation in BT474 cells. Chloropyramine hydrochloride treatment causes the overexpressed VEGFR-3 breast cancer cells to undergo apoptosis after 48 hours. More than 60% of BT474 cells experience apoptosis when exposed to 10 µM chloropyramine hydrochloride, indicating a dose-dependent effect. Treatment with 10 µM Chloropyramine hydrochloride for 48 hours increases apoptotic cell death in the cell line that overexpresses VEGFR-3 by four times (18% versus 76%, respectively) in our model cell lines MCF7-pcDNA3 and MCF7-VEGFR-3[1].
In vitro, Chloropyramine hydrochloride acts as a histamine H1 receptor antagonist. It inhibits VEGFR-3 and FAK biochemical functions. The compound exhibits anti-cholinergic and antispasmodic properties. Its receptor binding affinity and functional antagonism have been characterized in various in vitro systems. The compound is used in drug analysis research. |
| ln Vivo |
Chloropyramine hydrochloride causes both model systems to experience a sharp decline in tumor growth, with treated groups' tumor sizes being about 20% smaller than those of the vehicle control groups. Tumor growth is reduced by about 60% when doxorubicin is given at a dose of 3 mg/kg; at 0 mg/kg, tumor growth is unaffected. However, chloropyramine hydrochloride by itself only has a negligible impact (a 50% decrease in tumor growth). A prolonged anti-tumor effect (85% reduction in tumor growth) is achieved by the low-dose combination of doxorubicin and chloropyramine hydrochloride, which is superior to either drug alone[1].
In vivo, Chloropyramine hydrochloride is used to treat allergic conjunctivitis, allergic rhinitis, bronchial asthma, and other atopic diseases. It is a first-generation antihistamine with sedative effects due to CNS activity. The compound has anti-cholinergic and antispasmodic properties. It is available under brand names including Suprastin, Alergosan, and Sinopen. |
| Enzyme Assay |
The cells are cultured with or without Chloropyramine Hydrochloride, and then stained with either anti-FAK antibody 4.47, paxillin, or VEGFR-3. Alexa Fluor 546 secondary antibody is used for detection, and a combination of Alexa Fluor 488 and Alexa Fluor 546 secondary antibody is used for dual staining[1].
In vitro receptor binding assays for Chloropyramine hydrochloride involve measuring affinity for the histamine H1 receptor. Radioligand binding displacement studies are performed using membranes from cells expressing the H1 receptor. VEGFR-3 and FAK inhibition are assessed using kinase activity assays. Functional antagonism is assessed by measuring inhibition of histamine-induced calcium mobilization or other signaling. Assays are performed in appropriate buffer systems with positive controls. |
| Cell Assay |
The MTS assay measures the mitochondrial dehydrogenase activity of metabolically active cells in order to assess cell survival. In 96-well plates, 5.0×103 (100 µL) cells are plated and left to attach for the entire night. Each well receives the addition of 100 microliters of fresh media, either with or without chloropyramine hydrochloride. Cells receive treatment for a predetermined period of time. As directed by the manufacturer, the MTS assay is carried out[1].
In vitro cell-based assays for Chloropyramine hydrochloride are conducted in cells expressing the histamine H1 receptor. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Receptor antagonism is assessed by measuring inhibition of histamine-induced signaling. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive and negative controls. |
| Animal Protocol |
Five mice per group, aged five to six weeks, receive subcutaneous injections of BT474 and MCF7-VEGFR-3 cells at a concentration of 2 to 5×106 cells per 200 µL into their right flanks. The following day, following the intraperitoneal injection (IP) of cells once daily, treatment with chloropyramine hydrochloride is initiated. The volume of the tumor is computed using the formula length×width2×0.5, and the tumor size is measured three times per week. Once the tumor size reaches the protocol end point, or after 21 days of treatment, the animals are sacrificed. For the purpose of preparing proteins and RNA and doing cytochemistry, the tumor is removed, measured, and preserved[1].
Chloropyramine hydrochloride in vivo studies are conducted in animal models of allergic diseases. Animals are treated with the compound via oral administration or injection. Allergic responses such as skin reactions, airway inflammation, or anaphylaxis are assessed. For antispasmodic studies, smooth muscle contraction is assessed. Animals are monitored for clinical signs. Tissues and blood samples are collected for histopathological and biomarker analysis. Studies are conducted in accordance with institutional animal care guidelines. |
| ADME/Pharmacokinetics |
Chloropyramine hydrochloride (MW 326.26 g/mol, C16H20ClN3·HCl) is a first-generation antihistamine. It is soluble in DMSO and water. The compound is stable under recommended storage conditions. Chloropyramine hydrochloride is a histamine H1 receptor antagonist with anti-cholinergic and antispasmodic properties. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution have been characterized in clinical studies.
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| Toxicity/Toxicokinetics |
Chloropyramine hydrochloride is generally well-tolerated at therapeutic doses. The compound is a first-generation antihistamine with established safety profiles. It has sedative effects due to CNS activity. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation is available from clinical use data.
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| References | |
| Additional Infomation |
N'-[(4-chlorophenyl)methyl]-N,N-dimethyl-N'-(2-pyridyl)ethane-1,2-diamine is an aminopyridine drug. Clopidogrel is a first-generation antihistamine used in Eastern European countries to treat bronchial asthma, allergic rhinitis, allergic conjunctivitis, and other allergic reactions. It is also indicated for the treatment of angioedema, insect bite allergies, food and drug allergies, and anaphylactic shock. Indications: Used to treat allergic conjunctivitis, allergic rhinitis, bronchial asthma, and other atopic (allergic) diseases. Mechanism of Action: Clopidogrel binds to histamine H1 receptors. This blocks the effects of endogenous histamine, thereby temporarily relieving the negative symptoms caused by histamine. Pharmacodynamics: Clopidogrel is a competitive, reversible H1 receptor antagonist. It inhibits vasodilation, increased vascular permeability, and tissue edema associated with histamine release. In addition, clopidogrel also has certain anticholinergic properties. These effects, combined with its ability to cross the blood-brain barrier, can lead to side effects such as drowsiness, weakness, dizziness, fatigue, dry mouth, and constipation. In rare cases, visual impairment and increased intraocular pressure may also occur.
Chloropyramine hydrochloride is a first-generation antihistamine of the ethylenediamine class that acts as a potent histamine H1 receptor antagonist. It is used to treat allergic conjunctivitis, allergic rhinitis, bronchial asthma, and other atopic diseases. The compound also inhibits VEGFR-3 and FAK and has anti-cholinergic and antispasmodic properties. Its molecular formula is C16H20ClN3·HCl with a molecular weight of 326.26 g/mol.All applications are limited to non-human research use. |
| Molecular Formula |
C₁₆H₂₁CL₂N₃
|
|---|---|
| Molecular Weight |
326.26
|
| Exact Mass |
325.111
|
| Elemental Analysis |
C, 58.90; H, 6.49; Cl, 21.73; N, 12.88
|
| CAS # |
6170-42-9
|
| Related CAS # |
Chloropyramine; 59-32-5
|
| PubChem CID |
25295
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
413.5ºC at 760 mmHg
|
| Melting Point |
< 25 °C
60 °C |
| Flash Point |
203.9ºC
|
| LogP |
4.105
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
20
|
| Complexity |
264
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN(C)CCN(CC1=CC=C(Cl)C=C1)C2=NC=CC=C2.[H]Cl
|
| InChi Key |
VEYWWAGBHABATA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H20ClN3.ClH/c1-19(2)11-12-20(16-5-3-4-10-18-16)13-14-6-8-15(17)9-7-14;/h3-10H,11-13H2,1-2H3;1H
|
| Chemical Name |
N'-[(4-chlorophenyl)methyl]-N,N-dimethyl-N'-pyridin-2-ylethane-1,2-diamine;hydrochloride
|
| Synonyms |
Chloropyribenzamine hydrochloride; Halopyramine hydrochloride; Alergosan; Allergan hydrochloride; Nilfan; Sinopen; Suprastin
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 30~65 mg/mL (92~199.2 mM)
H2O: ~100 mg/mL (~306.5 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.38 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 20.8 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: ≥ 2.08 mg/mL (6.38 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (153.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0650 mL | 15.3252 mL | 30.6504 mL | |
| 5 mM | 0.6130 mL | 3.0650 mL | 6.1301 mL | |
| 10 mM | 0.3065 mL | 1.5325 mL | 3.0650 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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