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ICA-105665
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ICA-105665图片
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
PF-04895162
产品介绍
ICA-105665 (PF-04895162) 是一种有效的口服活性的神经元Kv7.2/7.3Kv7.3/7.5钾通道激动剂。ICA-105665 抑制肝线粒体功能和胆盐输出蛋白 (BSEP) 转运 (IC50为 311 μM). ICA-105665 可穿透血脑屏障并具有抗癫痫作用。
生物活性

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].

IC50& Target

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

体外研究
(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 (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].

体内研究
(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 mgkg[3].

Clinical Trial
分子量

355.34

性状

Solid

Formula

C19H15F2N3O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8142 mL14.0710 mL28.1421 mL
5 mM0.5628 mL2.8142 mL5.6284 mL
10 mM0.2814 mL1.4071 mL2.8142 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。