ICA 069673 Chemical Properties

Boiling point:

358.9±37.0 °C(Predicted)

Density 

1.539±0.06 g/cm3(Predicted)

storage temp. 

Sealed in dry,Room Temperature

solubility 

DNF:30.0(Max Conc. mg/mL);111.26(Max Conc. mM)
DMSO:36.24(Max Conc. mg/mL);134.4(Max Conc. mM)
Ethanol:30.25(Max Conc. mg/mL);112.18(Max Conc. mM)

pka

9.47±0.70(Predicted)

form 

Powder

color 

White to off-white

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)

InChIKey

IIBSHMFXVWTQSJ-UHFFFAOYSA-N

SMILES

O=C(C1=CC=C(F)C(F)=C1)NC2=CN=C(Cl)N=C2

Safety Information

WGK Germany 

WGK 3

Storage Class

11 - Combustible Solids

ICA 069673 Usage And Synthesis

Description

ICA 069673 is a heteromeric K_v7 channel activator. It is selective for K_v7.2/7.3 over K_v7.3/7.5 (EC₅₀s = 0.69 and 14.3 μM, respectively) and also activates K_v7.4, K_v7.5, and heteromeric K_v7.4/7.5 channels in a dose-dependent manner. ICA 069673 has no activity against hERG, Na_v1.5, and K_v7.1 cardiac ion channels (IC₅₀s = >30 μM). Oral administration of ICA 069673 increases latency to first tonic-clonic seizure in the rat maximal electroshock and pentylentetrazol-induced seizure models (ED₅₀s = 1.5 and <1 mg/kg, respectively). Formulations containing ICA 069673 are under clinical investigation for the treatment of epilepsy.

Uses

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[1][2].

storage

Room temperature

References

[1] Provence A, et al. The Novel KV7.2/KV7.3 Channel Opener ICA-069673 Reveals Subtype-Specific Functional Roles in Guinea Pig Detrusor Smooth Muscle Excitability and Contractility. J Pharmacol Exp Ther. 2015 Sep;354(3):290-301. DOI:10.1124/jpet.115.225268