| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
TASK-1-IN-1 targets the TASK-1 (TWIK-related acid-sensitive K+ channel 1) potassium channel. TASK-1 is a two-pore domain potassium channel that maintains resting membrane potential and regulates neuronal and cardiac excitability. The compound functions as a potent and selective TASK-1 inhibitor. It has no significant impact on other K+ channels.
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| ln Vitro |
TASK-1-IN-1 (compound F3) inhibits the growth and survivability of MCF-7 cancer cell lines but not TASK-1 knockout MCF-7 cells, suggesting that it functions through the TASK-1 channel [1].
In vitro, TASK-1-IN-1 is a potent TASK-1 inhibitor with an IC50 of 148 nM. It shows reduced inhibition of TASK-3 (IC50 = 1750 nM) and has no significant impact on other K+ channels. The compound's selectivity for TASK-1 over TASK-3 makes it a valuable tool for studying TASK-1-specific functions. |
| ln Vivo |
Specific in vivo activity data for TASK-1-IN-1 are not extensively reported. As a TASK-1 inhibitor, it modulates neuronal and cardiac excitability. It may be used in research on sleep apnea, atrial fibrillation, and pulmonary arterial hypertension.
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| Enzyme Assay |
The binding and inhibition of TASK-1 are measured using electrophysiological techniques such as patch-clamp recordings in cells expressing TASK-1 channels. TASK-1-IN-1 is applied at varying concentrations, and channel currents are measured to calculate IC50 values. Whole-cell or inside-out patch configurations are commonly used.
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: MCF-7 Cell Tested Concentrations: 10 μM Incubation Duration: 96 hrs (hours) Experimental Results: Approximately 45% anti-proliferative activity against cell line MCF-7. The cellular activity of TASK-1-IN-1 is evaluated in TASK-1-expressing cell lines. Cells are treated with the compound, and channel activity is measured using electrophysiological or fluorescence-based membrane potential assays. High-throughput screening using voltage-sensitive dyes can also be employed. |
| Animal Protocol |
In vivo efficacy of TASK-1-IN-1 would typically be evaluated in animal models of sleep apnea, atrial fibrillation, or pulmonary arterial hypertension. Animals would be administered the compound, and physiological parameters such as respiratory rate, heart rhythm, and blood pressure would be assessed.
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| ADME/Pharmacokinetics |
TASK-1-IN-1 has a molecular formula of C22H20N2O2 and a molecular weight of 344.41 g/mol. Its chemical name is 3-benzamido-N-(2-ethylphenyl)benzamide. Purity is 98%.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for TASK-1-IN-1 are limited. The compound is intended for research use only. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
TASK-1-IN-1 is a potent and selective TASK-1 inhibitor (IC50 = 148 nM). It is a valuable tool for studying TASK-1 channel function and its role in sleep apnea, atrial fibrillation, and pulmonary arterial hypertension. The compound also has potential anticancer/antitumor effects.
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| Molecular Formula |
C22H20N2O2
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|---|---|
| Molecular Weight |
344.406405448914
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| Exact Mass |
344.15
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| Elemental Analysis |
C, 76.72; H, 5.85; N, 8.13; O, 9.29
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| CAS # |
600125-11-9
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| PubChem CID |
3470140
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
473
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C=CC=C(C=1)NC(C1C=CC=CC=1)=O)NC1C=CC=CC=1CC
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| InChi Key |
MRIKKSSTVCDDDZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20N2O2/c1-2-16-9-6-7-14-20(16)24-22(26)18-12-8-13-19(15-18)23-21(25)17-10-4-3-5-11-17/h3-15H,2H2,1H3,(H,23,25)(H,24,26)
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| Chemical Name |
3-benzamido-N-(2-ethylphenyl)benzamide
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| Synonyms |
TASK-1-IN-1; TASK-1 blocker F3; TASK-1 Inhibitor F3; GLXC-26542
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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 : ~66.67 mg/mL (~193.58 mM)
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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 | 2.9035 mL | 14.5176 mL | 29.0352 mL | |
| 5 mM | 0.5807 mL | 2.9035 mL | 5.8070 mL | |
| 10 mM | 0.2904 mL | 1.4518 mL | 2.9035 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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