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| Targets |
H1-histamine receptor (antagonist). Oxatomide is an H1-histamine receptor antagonist. H1 receptors are G protein-coupled receptors that mediate the effects of histamine, a key mediator of allergic reactions. By antagonizing H1 receptors, Oxatomide blocks histamine-induced effects such as vasodilation, bronchoconstriction, and smooth muscle contraction. The compound exhibits both antihistamine and anti-inflammatory properties. Its novel biphasic mode of action distinguishes it from other antihistamines. Oxatomide is an orally active anti-allergic agent.
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| ln Vitro |
Oxatomide demonstrates H1-histamine receptor antagonist activity in vitro. The compound binds to H1 receptors and blocks histamine-induced signaling. It exhibits both antihistamine and anti-inflammatory properties. Its anti-allergic effects have been characterized in various in vitro assays. Oxatomide is an orally active anti-allergic agent. The compound may be useful in managing asthma. Detailed quantitative activity data (e.g., IC50, Ki) are not extensively available in publicly accessible sources.
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| ln Vivo |
Oxatomide is an orally active anti-allergic agent that has been studied in vivo for its effects on allergic conditions. The compound exhibits therapeutic effects against asthma and vulvar lichen sclerosus. It has both antihistamine and anti-inflammatory properties. Oxatomide may be useful in managing asthma. Detailed in vivo pharmacokinetic and pharmacodynamic data are available from preclinical and clinical studies. Oxatomide is for research use only and is not for human therapeutic use.
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| Enzyme Assay |
H1-histamine receptor binding assays are performed using membranes prepared from cells expressing recombinant H1 receptors or from tissue sources. Radioligand binding studies use [³H]-pyrilamine or [³H]-mepyramine as labeled ligands. Membrane preparations are incubated with varying concentrations of Oxatomide and a fixed concentration of radioligand in binding buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl₂, 1 mM EDTA) for 60-120 minutes at room temperature. Non-specific binding is determined using excess unlabeled pyrilamine or mepyramine. Bound radioactivity is measured by scintillation counting after filtration through GF/B filters. IC50 and Ki values are calculated by non-linear regression. Functional assays measure H1 receptor-mediated calcium mobilization.
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| Cell Assay |
Cellular H1 receptor antagonism is evaluated in cell lines expressing recombinant H1 receptors (e.g., HEK-293 cells). Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with Oxatomide at various concentrations. Functional assays measure receptor-mediated calcium mobilization in response to histamine stimulation. The compound's antagonist activity is assessed by its ability to inhibit histamine-induced calcium responses. Cell viability is assessed using MTT or LDH assays. Each experiment includes known H1 antagonists (e.g., diphenhydramine) as positive controls and vehicle controls.
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| Animal Protocol |
In vivo efficacy of Oxatomide is evaluated in animal models of allergic diseases, such as asthma and allergic rhinitis. The compound is administered orally at doses determined by preclinical studies. Airway hyperresponsiveness is assessed by methacholine challenge. Inflammatory cell infiltration and cytokine levels are measured in bronchoalveolar lavage fluid. In models of vulvar lichen sclerosus, the compound's effects on inflammation and tissue remodeling are assessed. Sample sizes typically range from 6-10 animals per group. Clinical studies have been conducted for asthma and other allergic conditions.
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| ADME/Pharmacokinetics |
Molecular Weight: 426.55. Formula: C27H30N4O. CAS No.: 60607-34-3. IUPAC Name: 1-[3-[4-(Diphenylmethyl)-1-piperazinyl]propyl]-1,3-dihydro-2H-benzimidazol-2-one. Synonyms: Oxatomide, KW-4354. Appearance: White powder. Melting Point: 153.60°C. Purity: 99%. Solubility: DMSO: soluble. Storage: Refrigerator. Oxatomide is an orally active anti-allergic agent and H1-histamine receptor antagonist.
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| Toxicity/Toxicokinetics |
Oxatomide has been evaluated for toxicity. It is a poison by ingestion, intraperitoneal, and intravenous routes. LD50 in guinea pigs, mice, rats (mg/kg): 320, >2560, >2560 orally; 23, 27, 30 i.v.. It is an experimental teratogen with experimental reproductive effects. The compound is for research use only and is not for human therapeutic use.
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| References | |
| Additional Infomation |
Oxatomide belongs to the benzimidazole class of compounds, with the structure 1,3-dihydro-2H-benzimidazole-2-one, where the 1-position is substituted with a 3-[4-(diphenylmethyl)piperazin-1-yl]propyl group. It is an anti-allergic drug with anti-aging, H1 receptor antagonistic, anti-allergic, anti-inflammatory, and serotonin antagonistic effects. It is an N-alkylpiperazine compound, belonging to the benzimidazole and diarylmethane classes. Oxatomide has been used in clinical trials investigating the treatment of Duchenne muscular dystrophy.
Oxatomide is also known as KW-4354. Its IUPAC name is 1-[3-[4-(Diphenylmethyl)-1-piperazinyl]propyl]-1,3-dihydro-2H-benzimidazol-2-one. Oxatomide is an orally active anti-allergic agent that is structurally related to cinnarizine and has a novel biphasic mode of action. It is an H1-histamine receptor antagonist with both antihistamine and anti-inflammatory properties. Oxatomide exhibits therapeutic effects against asthma and vulvar lichen sclerosus. No regulatory approvals have been reported. Oxatomide is for research use only. |
| Molecular Formula |
C27H30N4O
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| Molecular Weight |
426.5533
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| Exact Mass |
426.242
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| CAS # |
60607-34-3
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| PubChem CID |
4615
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| Appearance |
White to off-white solid powder
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| Density |
1.175 g/cm3
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| Boiling Point |
621.1ºC at 760 mmHg
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| Melting Point |
153.60C
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| Flash Point |
329.4ºC
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| Index of Refraction |
1.619
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| LogP |
4.002
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
32
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| Complexity |
575
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BAINIUMDFURPJM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H30N4O/c32-27-28-24-14-7-8-15-25(24)31(27)17-9-16-29-18-20-30(21-19-29)26(22-10-3-1-4-11-22)23-12-5-2-6-13-23/h1-8,10-15,26H,9,16-21H2,(H,28,32)
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| Chemical Name |
3-[3-(4-benzhydrylpiperazin-1-yl)propyl]-1H-benzimidazol-2-one
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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 |
| 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) |
DMSO : ~250 mg/mL (~586.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.88 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 (4.88 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 (4.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3444 mL | 11.7220 mL | 23.4439 mL | |
| 5 mM | 0.4689 mL | 2.3444 mL | 4.6888 mL | |
| 10 mM | 0.2344 mL | 1.1722 mL | 2.3444 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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