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ICA069673

Cat. No. M5302
ICA069673 Structure
Synonym:

ICA069673

Size Price Availability Quantity
10mg USD 180  USD180 In stock
50mg USD 720  USD720 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: 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. 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).

Protocol
Cell Experiment
Cell lines DSM cells
Preparation method For the first protocol, continuous stimulation of 10-Hz EFS frequency was delivered at 1-minute intervals and a stable baseline and amplitude were reached prior to applying increasing concentrations of ICA-069673 (100 nM–30 µM). In the second EFS protocol, we applied incremental EFS stimulation frequencies (3.5, 5, 7.5, 10, 12.5, 15, 20, 30, 40, and 50 Hz) at 3-minute intervals for a control period, and then again in the presence of a single concentration of ICA-069673 (either 3 or 10 µM).
Concentrations 100 nM–30 µM
Incubation time
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 269.63
Formula C11H6ClF2N3O
CAS Number 582323-16-8
Purity >98%
Solubility ≥ 34 mg/mL in DMSO
Storage at -20°C
References

[1] Aaron Provence, et al. J Pharmacol Exp Ther. The Novel KV7.2/KV7.3 Channel Opener ICA-069673 Reveals Subtype-Specific Functional Roles in Guinea Pig Detrusor Smooth Muscle Excitability and Contractility

[2] Brueggemann LI, et al. Mol Pharmacol. Differential activation of vascular smooth muscle Kv7.4, Kv7.5, and Kv7.4/7.5 channels by ML213 and ICA-069673.

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Keywords: ICA069673, ICA069673 supplier, Potassium Channel, inhibitors

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