ICA-105665

ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM) . ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects[1][2][3][4].

Product Specifications

CAS Number

[2694728-63-5]

Product Name Alternative

PF-04895162

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ica-105665.html

Concentration

10mM

Purity

99.85

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(NN1C(C2CC2)=NC3=C(C=CC(F)=C3)C1=O)CC4=CC=C(F)C=C4

Molecular Formula

C19H15F2N3O2

Molecular Weight

355.34

Precautions

H302, H315, H319, H335

References & Citations

[1] Aleo MD, et al. Phase I study of PF‐04895162, a Kv7 channel opener, reveals unexpected hepatotoxicity in healthy subjects, but not rats or monkeys: clinical evidence of disrupted bile acid homeostasis. Pharmacol Res Perspect. 2019 Feb;7 (1) :e00467.|[2]Generaux G, et al. Quantitative systems toxicology (QST) reproduces species differences in PF-04895162 liver safety due to combined mitochondrial and bile acid toxicity. Pharmacol Res Perspect. 2019 Oct 9;7 (6) :e00523.|[3]Kasteleijn-Nolst Trenité DG, et al. Kv7 potassium channel activation with ICA-105665 reduces photoparoxysmal EEG responses in patients with epilepsy. Epilepsia. 2013 Aug;54 (8) :1437-43.|[4]Bialer M, et al. Progress report on new antiepileptic drugs: a summary of the Eleventh Eilat Conference (EILAT XI) . Epilepsy Res. 2013 Jan;103 (1) :2-30.