| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
ICA-069673 (ICA73) is a selective KCNQ2/Q3 potassium channel activator with IC50 of 0.69 μM. KCNQ2 (Kv7.2) and KCNQ3 (Kv7.3) are voltage-gated K(+) channel subunits that underlie the neuronal M current. In humans, mutations in these genes lead to a rare form of neonatal epilepsy, suggesting that KCNQ2/Q3 channels may be attractive targets for novel antiepileptic drugs. ICA069673 acts on a binding site in the voltage-sensing domain that is distinct from the putative retigabine (a KCNQ voltage-gated potassium channel opener that was recently approved as an add-on therapeutic for patients with drug-resistant epilepsy) site in the channel pore. ICA069673 has two separable effects on KCNQ channel activity.
| ln Vitro |
In guinea pig DSM breakaway strips, ICA-069673 (100 nM-30 μM) dose-dependently suppresses spontaneous phasic contractions, contractions elicited by pharmacology, and contractions triggered neurally by 10 Hz EFS [1]. In guinea pig DSM separation strips, ICA-069673 (3 μM, 10 μM) suppresses the contraction of the DSM tetanic muscle elicited by 20 mM KCl [1].
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Animal Protocol |
|
||
| References |
| Molecular Formula |
C11H6CLF2N3O
|
|
|---|---|---|
| Molecular Weight |
269.64
|
|
| Exact Mass |
269.017
|
|
| CAS # |
582323-16-8
|
|
| Related CAS # |
|
|
| PubChem CID |
10149311
|
|
| Appearance |
White to off-white solid powder
|
|
| LogP |
3.044
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
5
|
|
| Rotatable Bond Count |
2
|
|
| Heavy Atom Count |
18
|
|
| Complexity |
300
|
|
| Defined Atom Stereocenter Count |
0
|
|
| InChi Key |
IIBSHMFXVWTQSJ-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C11H6ClF2N3O/c12-11-15-4-7(5-16-11)17-10(18)6-1-2-8(13)9(14)3-6/h1-5H,(H,17,18)
|
|
| Chemical Name |
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.27 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
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 (9.27 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (9.27 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7086 mL | 18.5432 mL | 37.0865 mL | |
| 5 mM | 0.7417 mL | 3.7086 mL | 7.4173 mL | |
| 10 mM | 0.3709 mL | 1.8543 mL | 3.7086 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.
ICA069673 (ICA73 ) exhibits subtype‐specificity for KCNQ2 over KCNQ3 channels. |
|---|
ICA73 potentiates KCNQ2 currents and induces a large hyperpolarizing shift of the conductance–voltage relationshipJ Physiol.2017 Feb 1;595(3):663-676. |
Substitution of KCNQ3 VSD into KCNQ2 alters channel sensitivity to ICA73.J Physiol.2017 Feb 1;595(3):663-676. |
Rubidium efflux screen identifies two S3 mutations that diminish ICA73 response.J Physiol.2017 Feb 1;595(3):663-676. |
|---|
 Functional characterization of KCNQ2[F168L] mutant channels
Functional characterization of KCNQ2[A181P] mutant channels illustrates the separable nature of current potentiation and gating shiftJ Physiol.2017 Feb 1;595(3):663-676. |
ICA73‐insensitive mutants do not perturb RTG sensitivity
ICA73‐sensitivity can be transferred into KCNQ3 via point mutations in the voltage sensorJ Physiol.2017 Feb 1;595(3):663-676. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
