1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. ICA-105665

ICA-105665 (Synonyms: PF-04895162)

Cat. No.: HY-125469
Handling Instructions

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.

For research use only. We do not sell to patients.

ICA-105665 Chemical Structure

ICA-105665 Chemical Structure

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Description

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].

IC50 & Target

Kv7.2/7.3 and Kv7.3/7.5 potassium channels[1][2]

In Vitro

ICA-105665 (PF-04895162) does not display potent cytotoxic properties in THLE and HepG2 cell lines (IC50 ~192 μM and 130 μM after 72 hours, respectively) or in human hepatocytes (AC50 for cell loss at 48 hours was >125 μM based on results in three assessments in two different human hepatocyte lots (LBN and HU4165)[1].
Mitochondrial respiratory reserve is compromised in human hepatocytes treated with ICA-105665 (PF-04895162) at concentrations >11 μM for 25 minutes[1].

In Vivo

For ICA-105665 (PF-04895162), in a 7-day rat toxicity study, dose-dependent alanine aminotransferase (ALT) elevations, potentially indicative of liver toxicity, were observed. However, no histological evidence of liver injury was identified, and ALT elevations were not confirmed in a repeat 7-day study. Further, 28 day and 6 month toxicity studies in rats were negative for transaminase elevations and liver toxicity, and toxicity studies up to 9 months duration in cynomolgus monkeys were also negative[2].
ICA-105665 (PF-04895162) has demonstrated broad spectrum antiseizure activity in multiple animal models including maximal electroshock, 6 Hz seizures, pentylenetetrazole, and electrical kindling at doses from <1 to 5 mg/kg[3].

Molecular Weight

355.34

Formula

C₁₉H₁₅F₂N₃O₂

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ICA-105665PF-04895162ICA105665ICA 105665PF04895162PF 04895162Potassium ChannelKcsAAntiepilepticmitochondrialBSEPtransaminasebileacidsneuronalKv7KCNQ2/3KCNQ3/5BBBInhibitorinhibitorinhibit

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ICA-105665
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HY-125469
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