ICA 069673 |
رقم الكتالوجGC16447
One-Click Copy Product Info
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ICA 069673 هو منشط لقناة البوتاسيوم KCNQ2 / Q3 مع IC50 0.69 ميكرومتر.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 582323-16-8
Sample solution is provided at 25 µL, 10mM.
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ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM.
ICA-069673 is found to be 20-fold selective for KCNQ2/Q3 over KCNQ3/Q5 and has no measurable activity against a panel of cardiac ion channels (IC50 values > 30 μM for hERG, Nav1.5, L type channels, and KCNQ1) as well as no activity on GABA(A) gated channels at 10 μM[1]. ICA-069673 exhibits much stronger effects on KCNQ2 channels, including a large hyperpolarizing shift of the voltage-dependence of activation, an 2-fold enhancement of peak current and pronounced subtype specificity for KCNQ2 over KCNQ3. Based on ICA73 sensitivity of chimeric constructs of the transmembrane segments of KCNQ2 and KCNQ3, this drug appears to interact with the KCNQ2 voltage sensor (S1-S4)[2].
References:
[1]. Wickenden AD, et al. N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243): a novel, selective KCNQ2/Q3 potassium channel activator. Mol Pharmacol. 2008 Mar;73(3):977-86. Epub 2007 Dec 18.
[2]. Wang AW, et al. Sequence determinants of subtype-specific actions of KCNQ channel openers. J Physiol. 2017 Feb 1;595(3):663-676.
| Cas No. | 582323-16-8 | SDF | |
| Chemical Name | (Z)-N-(2-chloropyrimidin-5-yl)-3,4-difluorobenzimidic acid | ||
| Canonical SMILES | ClC1=NC=C(/N=C(O)/C2=CC(F)=C(F)C=C2)C=N1 | ||
| Formula | C11H6ClF2N3O | M.Wt | 269.63 |
| الذوبان | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7088 mL | 18.5439 mL | 37.0879 mL |
| 5 mM | 741.8 μL | 3.7088 mL | 7.4176 mL |
| 10 mM | 370.9 μL | 1.8544 mL | 3.7088 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)