ICA-069673
Based on 3 publication(s) in Google Scholar
ICA-069673 is a KCNQ2/Q3 potassium channel activator. ICA-069673 demonstrates greater selectivity for KV7.2/7.3 over KV7.3/KV7.5, with EC50s of 0.69 μM and 14.3 μM, respectively. ICA-069673 inhibits spontaneous phasic and nerve-evoked contractions in guinea pig detrusor smooth muscle (DSM). ICA-069673 also decreases the global intracellular Ca(2+) concentration in DSM cells.
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- Purity: 99.20%
- CAS No.: 582323-16-8
- 화학식: C11H6ClF2N3O
- 분자량:269.63
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ICA-069673
More
Biological Activity
IC50: 0.69 μM (KV7.2/7.3), 14.3 μM (KV7.3/7.5)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.69 μM
Compound: 51, ICA-069673
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Agonist activity at KCNQ2/KCNQ3 expressed in CHO cells assessed as increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
Agonist activity at KCNQ2/KCNQ3 expressed in CHO cells assessed as increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
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[PMID: 24900334] |
| CHO | EC50 |
14.3 μM
Compound: 51, ICA-069673
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Agonist activity at KCNQ3/KCNQ5 expressed in CHO cells increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
Agonist activity at KCNQ3/KCNQ5 expressed in CHO cells increase in KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
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[PMID: 24900334] |
| CHO | IC50 |
>100 μM
Compound: 51, ICA-069673
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Antagonist activity at KCNQ1/MINK expressed in CHO cells assessed as inhibition of KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
Antagonist activity at KCNQ1/MINK expressed in CHO cells assessed as inhibition of KCl-induced 86Rb+ efflux incubated for 10 mins prior to KCl-induction by liquid scintillation counting
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[PMID: 24900334] |
ICA-069673 (100 nM-30 μM) dose-dependently inhibits spontaneous phasic contraction, pharmacologically induced contraction, and 10 Hz EFS induced nerve-evoked contraction, in guinea pig DSM isolated strips[1].
ICA-069673 (3 μM, 10 μM) inhibits 20 mM KCl induced DSM tonic contractions in guinea pig DSM isolated strips[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 582323-16-8
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Appearance Solid
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분자량 269.63
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화학식 C11H6ClF2N3O
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Color White to off-white
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SMILES
O=C(NC1=CN=C(Cl)N=C1)C2=CC=C(F)C(F)=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Functional characterization and in vitro pharmacological rescue of KCNQ2 pore mutations associated with epileptic encephalopathy. [Abstract]2023 Aug;44(8):1589-1599. PMID: 36932231 -
Am J Physiol Cell Physiol
M2 muscarinic receptor-dependent contractions of airway smooth muscle are mediated by inhibition of Kv7 channels. [Abstract]2026 Mar 5. PMID: 41784087 -
용액&용해도
DMSO : 50 mg/mL (185.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (9.27 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (9.27 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7088 mL | 18.5439 mL | 37.0879 mL | 92.7197 mL |
| 5 mM | 0.7418 mL | 3.7088 mL | 7.4176 mL | 18.5439 mL | |
| 10 mM | 0.3709 mL | 1.8544 mL | 3.7088 mL | 9.2720 mL | |
| 15 mM | 0.2473 mL | 1.2363 mL | 2.4725 mL | 6.1813 mL | |
| 20 mM | 0.1854 mL | 0.9272 mL | 1.8544 mL | 4.6360 mL | |
| 25 mM | 0.1484 mL | 0.7418 mL | 1.4835 mL | 3.7088 mL | |
| 30 mM | 0.1236 mL | 0.6181 mL | 1.2363 mL | 3.0907 mL | |
| 40 mM | 0.0927 mL | 0.4636 mL | 0.9272 mL | 2.3180 mL | |
| 50 mM | 0.0742 mL | 0.3709 mL | 0.7418 mL | 1.8544 mL | |
| 60 mM | 0.0618 mL | 0.3091 mL | 0.6181 mL | 1.5453 mL | |
| 80 mM | 0.0464 mL | 0.2318 mL | 0.4636 mL | 1.1590 mL | |
| 100 mM | 0.0371 mL | 0.1854 mL | 0.3709 mL | 0.9272 mL |
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