ICA-105665 (PF-04895162) is a potent and orally active neuronalKv7.2/7.3andKv7.3/7.5 potassium channelsopener. ICA-105665 inhibits liver mitochondrial function andbile salt export protein (BSEP)transport (IC₅₀of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects^[1][2][3][4].

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

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 (AC₅₀for 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].

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 mgkg^[3].

355.34

Solid

C₁₉H₁₅F₂N₃O₂

Room temperature in continental US; may vary elsewhere.

DMSO : 250 mg/mL(703.55 mM;Need ultrasonic)

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