| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Imoxiterol acts as a β-adrenergic receptor agonist, with selectivity for the β2-adrenoceptor subtype. The β2-adrenoceptor is predominantly expressed in airway smooth muscle, and its activation leads to bronchodilation. Imoxiterol’s mechanism involves binding to this receptor and catalyzing the conversion of ATP to cyclic AMP, which results in smooth muscle relaxation. Its selectivity for the β2 subtype over β1 is a key feature for its intended use in respiratory research.
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| ln Vitro |
In vitro, Imoxiterol demonstrates potent relaxation of pre-contracted airway smooth muscle preparations, indicative of its functional β2-agonist activity. It has an EC50 of 3.2 ± 0.9 μg/mL in histamine-challenged guinea-pig models. Importantly, it shows negligible PPARγ transactivation (EC50 >15 μM), ensuring a clean β2-signaling attribution in metabolic research and eliminating confounding off-target effects in studies involving adipocytes or insulin sensitization.
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| ln Vivo |
In vivo, Imoxiterol is studied for its ability to relax airway smooth muscles, making it easier to breathe. Its long-acting profile suggests sustained bronchodilation in animal models of airway hyperresponsiveness. It provides a duration of action exceeding 90 minutes, which supports extended experimental protocols without the need for repeat dosing. This pharmacokinetic feature makes it a useful tool for prolonged studies of bronchoprotection.
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| Enzyme Assay |
β2-adrenoceptor agonist activity is typically confirmed using membrane preparations from cells expressing the human β2-adrenoceptor. Radioligand binding assays with [³H]-dihydroalprenolol are performed to determine the affinity (Ki) of Imoxiterol for the receptor. Competition curves are generated by incubating membranes with increasing concentrations of the compound.
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| Cell Assay |
The functional activity of Imoxiterol is evaluated in vitro using cells (e.g., CHO cells) stably expressing the human β2-adrenoceptor. The compound's ability to stimulate cAMP accumulation is measured as a readout of receptor activation. A dose-response curve is generated, and the EC50 for cAMP production is calculated to determine its potency.
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| Animal Protocol |
In vivo efficacy is assessed in animal models of bronchoconstriction, such as histamine-challenged guinea pigs. In these models, Imoxiterol is typically administered via nebulization. Airway resistance is measured following administration of a bronchoconstrictor, and the ability of the compound to prevent or reverse this constriction is evaluated over time to determine its duration of action, which has been shown to exceed 90 minutes.
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| ADME/Pharmacokinetics |
Based on its structural class as a β2-agonist and its intended use for inhalation, Imoxiterol is expected to have a rapid onset and a prolonged duration of action. It is designed for high local lung exposure and low systemic bioavailability, which would minimize systemic side effects. The compound's LogP value of 3.243 suggests moderate lipophilicity, which is typical for molecules designed for pulmonary delivery.
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| Toxicity/Toxicokinetics |
As with other β2-agonists, potential toxicities of Imoxiterol may include cardiovascular effects such as tachycardia and palpitations, as well as tremor and hypokalemia, particularly at high systemic doses. Its negligible activity at PPARγ reduces the risk of metabolic side effects that could confound research data.
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| Additional Infomation |
Imoxiterol is primarily a research compound developed for the treatment of respiratory diseases like asthma and COPD. It is structurally related to other long-acting β2-agonists (LABAs) but did not advance to widespread clinical use. It remains a valuable tool for studying β2-adrenoceptor pharmacology, particularly in the context of structure-kinetic relationships and the development of new bronchodilators.
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| Molecular Formula |
C20H25N3O3
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|---|---|
| Molecular Weight |
355.438
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| Exact Mass |
355.19
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| CAS # |
88578-07-8
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| PubChem CID |
65665
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| Appearance |
Light brown to brown solid powder
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| Density |
1.23g/cm3
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| Boiling Point |
590.3ºC at 760 mmHg
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| Flash Point |
310.8ºC
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| Index of Refraction |
1.608
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| LogP |
3.243
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
26
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| Complexity |
425
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NKKPVWPMPWLEMY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H25N3O3/c1-14(9-10-23-13-22-16-5-3-4-6-17(16)23)21-12-19(25)15-7-8-18(24)20(11-15)26-2/h3-8,11,13-14,19,21,24-25H,9-10,12H2,1-2H3
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| Chemical Name |
4-[2-[4-(benzimidazol-1-yl)butan-2-ylamino]-1-hydroxyethyl]-2-methoxyphenol
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| Synonyms |
RP58802B; RP 58802B; Imoxiterol
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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 | 2.8134 mL | 14.0671 mL | 28.1341 mL | |
| 5 mM | 0.5627 mL | 2.8134 mL | 5.6268 mL | |
| 10 mM | 0.2813 mL | 1.4067 mL | 2.8134 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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