| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary target is the histamine H1 receptor, a Gq-coupled receptor that mediates allergic responses including vasodilation, increased vascular permeability, and bronchoconstriction. Embramine competitively antagonizes histamine binding to H1 receptors, blocking downstream phospholipase C activation and calcium mobilization. It also exhibits anticholinergic activity, likely through muscarinic acetylcholine receptor antagonism, contributing to its side effect profile.
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|---|---|
| ln Vitro |
Embramine is a first-generation H1-antihistamine with anticholinergic properties. In clinical studies of chronic idiopathic urticaria, the potency sequence of seven common H1 antagonists was established as cyproheptadine > hydroxyzine > chlorpheniramine > embramine > promethazine > dimethindene > dexchlorpheniramine. Among 11 tested antihistamines, only bromadryl (embramine), clemastine, and dithiaden effectively inhibited iNOS expression in LPS-stimulated macrophages.
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| ln Vivo |
In vivo, Embramine is used for allergic conditions including urticaria and rhinitis. It is orally active and produces antihistaminergic effects. As a first-generation antihistamine, it crosses the blood-brain barrier and causes sedation. Typical doses range from 25-50 mg administered 2-3 times daily. It is effective in reducing whealing and itching in chronic urticaria.
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| Enzyme Assay |
Radioligand binding assays use membranes from cells expressing recombinant human H1 receptors. The assay employs a radiolabeled H1 antagonist such as [3H]pyrilamine (mepyramine). Embramine is incubated with membranes and tracer in assay buffer for 60-90 minutes at 25°C. Bound radioactivity is separated by filtration and quantified by scintillation counting. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell-based assays for H1 receptor antagonism use U937 cells or CHO-K1 cells expressing recombinant H1 receptors. Cells are treated with Embramine (0.1-100 µM) and stimulated with histamine. Intracellular calcium mobilization is measured using Fluo-4 fluorescence. Inflammatory cytokine production (TNF-α, IL-6) in LPS-stimulated macrophages is measured by ELISA.
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| Animal Protocol |
In vivo, Embramine is tested in animal models of allergy and inflammation. A typical protocol involves oral administration (1-30 mg/kg) in guinea pigs or rats. Histamine-induced bronchoconstriction is assessed by measuring airway resistance. Passive cutaneous anaphylaxis is evaluated by Evans blue dye extravasation. Sedation is assessed using locomotor activity monitoring.
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| Additional Infomation |
Embramine is a diarylmethane.
|
| Molecular Formula |
C18H22NOBR
|
|---|---|
| Molecular Weight |
348.27738
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| Exact Mass |
347.088
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| CAS # |
3565-72-8
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| Related CAS # |
Embramine hydrochloride;13977-28-1
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| PubChem CID |
19105
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.234g/cm3
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| Boiling Point |
405.8ºC at 760mmHg
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| Flash Point |
199.2ºC
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| Index of Refraction |
1.561
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| LogP |
4.29
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| tPSA |
12.47
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| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
|
| Heavy Atom Count |
21
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| Complexity |
296
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(C1=CC=CC=C1)(C2=CC=C(Br)C=C2)OCCN(C)C
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| InChi Key |
URSRSKSNFPUKGH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H22BrNO/c1-18(21-14-13-20(2)3,15-7-5-4-6-8-15)16-9-11-17(19)12-10-16/h4-12H,13-14H2,1-3H3
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| Chemical Name |
2-[1-(4-bromophenyl)-1-phenylethoxy]-N,N-dimethylethanamine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.8713 mL | 14.3563 mL | 28.7125 mL | |
| 5 mM | 0.5743 mL | 2.8713 mL | 5.7425 mL | |
| 10 mM | 0.2871 mL | 1.4356 mL | 2.8713 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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