| 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 |
| Targets |
1-EBIO targets potassium channels, including intermediate-conductance calcium-activated potassium channels (IK-1 or KCa3.1), small-conductance calcium-activated potassium channels (SK), and the cystic fibrosis transmembrane conductance regulator (CFTR). It also modulates voltage-gated potassium channels KCNQ2. By activating these channels, 1-EBIO enhances potassium conductance, leading to membrane hyperpolarization. This hyperpolarization increases the driving force for calcium influx and modulates cellular excitability. In epithelial cells, 1-EBIO-induced KCa channel activation stimulates Cl⁻ secretion. Its ability to modulate multiple potassium channel types makes it a valuable tool for studying potassium channel function, epithelial transport, and vascular biology.
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| ln Vitro |
In vitro, 1-EBIO activates epithelial KCa channels, stimulating a large and sustained transepithelial Cl⁻ secretion response in T84 monolayers. In aortic valve endothelial cells, it induces hyperpolarization to the same extent as acetylcholine. 1-EBIO also activates CFTR, SK, and IK1 channels. Its activity is concentration-dependent, with effective concentrations typically ranging from 1 to 1000 µM. In electrophysiological studies, 1-EBIO increases potassium currents in patch-clamp recordings. Its ability to modulate multiple potassium channel types makes it a valuable tool for studying potassium channel function, epithelial transport, and vascular biology. Detailed EC50 values for specific channels are available in published literature.
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| ln Vivo |
In vivo, 1-EBIO has been used in animal studies to investigate the role of potassium channels in various physiological processes. However, detailed in vivo efficacy data are limited in publicly available sources. The compound's ability to activate KCa channels and modulate epithelial transport may have implications for gastrointestinal and respiratory diseases. 1-EBIO is primarily used as a research tool for studying potassium channel function and epithelial transport. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro potassium channel activation assay for 1-EBIO typically uses patch-clamp electrophysiology on cells expressing specific potassium channels (e.g., KCa3.1, SK, or KCNQ2). Cells are treated with varying concentrations of the test compound (typically 1 to 1000 µM), and potassium currents are recorded. The increase in current amplitude is used to quantify channel activation. For epithelial transport studies, T84 monolayers are mounted in Ussing chambers, and short-circuit current (Isc) is measured to assess Cl⁻ secretion. For endothelial cell studies, membrane potential is measured using fluorescent voltage-sensitive dyes or patch-clamp recordings. Positive controls (e.g., known KCa channel activators) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, epithelial cells (e.g., T84, Calu-3) or endothelial cells are treated with 1-EBIO at concentrations ranging from 1 to 1000 µM for 1-24 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Membrane potential is measured using fluorescent voltage-sensitive dyes. Intracellular calcium levels are measured using fluorescent calcium indicators. For Cl⁻ secretion studies, cells are grown on permeable supports, and transepithelial resistance and short-circuit current are measured in Ussing chambers. For mechanism studies, the effects of the compound on potassium channel expression and phosphorylation are assessed by Western blotting. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo studies, 1-EBIO may be administered to rodents via intraperitoneal injection or oral gavage at doses ranging from 1 to 50 mg/kg. However, specific in vivo protocols for 1-EBIO are not well-documented in publicly available sources. The compound may be used in models of epithelial transport, vascular function, or neurological disorders. All animal procedures should be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of 1-EBIO have been partially characterized. The compound has a molecular weight of 162.19 and is a small, polar molecule. Following intraperitoneal or oral administration, the compound shows moderate absorption with a Tmax of 0.5-1 hour. Plasma half-life is estimated to be 1-2 hours. The compound distributes into tissues including brain, liver, and kidney. Metabolism is primarily hepatic, with CYP450-mediated oxidation and conjugation as major pathways. The compound is eliminated primarily via renal excretion. Oral bioavailability is limited due to first-pass metabolism. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of 1-EBIO are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
1-Ethyl-2-benzimidazolinone is a member of the imidazole class of compounds.
1-EBIO is a potassium channel modulator that activates epithelial KCa channels, CFTR, SK, and IK1 channels. It stimulates Cl⁻ secretion in epithelial cells and induces hyperpolarization in endothelial cells. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use only. Its ability to modulate multiple potassium channel types makes it a valuable tool for studying potassium channel function, epithelial transport, and vascular biology. |
| Molecular Formula |
C9H10N2O
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|---|---|
| Molecular Weight |
162.1885
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| Exact Mass |
162.079
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| CAS # |
10045-45-1
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| PubChem CID |
82320
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| Appearance |
Light yellow to light brown solid powder
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| Density |
1.161±0.06 g/cm3
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| Melting Point |
122 ºC
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| Index of Refraction |
1.566
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| LogP |
1.39
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
12
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| Complexity |
193
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CXUCKELNYMZTRT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H10N2O/c1-2-11-8-6-4-3-5-7(8)10-9(11)12/h3-6H,2H2,1H3,(H,10,12)
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| Chemical Name |
3-ethyl-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 : ~100 mg/mL (~616.56 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (15.41 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 25.0 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: ≥ 2.5 mg/mL (15.41 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 25.0 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: ≥ 2.5 mg/mL (15.41 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 | 6.1656 mL | 30.8280 mL | 61.6561 mL | |
| 5 mM | 1.2331 mL | 6.1656 mL | 12.3312 mL | |
| 10 mM | 0.6166 mL | 3.0828 mL | 6.1656 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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