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ICA-105665

产品编号 T11606 CAS 2694728-63-5

别名: PF-04895162

ICA-105665 (PF-04895162) 是一种有效的口服活性的神经元 Kv7.2/7.3和 Kv7.3/7.5钾通道激动剂。ICA-105665 在人肝细胞中具有低细胞毒性潜力，但抑制肝线粒体功能和胆盐输出蛋白 (BSEP) 转运 (IC50为 311 μM)。ICA-105665 可穿透中枢神经系统 (CNS)并具有抗癫痫作用。

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ICA-105665, CAS 2694728-63-5

规格	价格/CNY		货期	数量
100 mg	￥ 11,996		10-14周
200 mg	￥ 17,997		10-14周

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	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 had low cytotoxic potential in human hepatocytes but inhibited liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the central nervous system (CNS) and has antiseizure effects[1][2][3][4].
体外活性	ICA-105665 (PF-04895162) does not exhibit strong cytotoxic properties in THLE and HepG2 cell lines (IC 50 ~192 μM and 130 μM after 72 hours, respectively) or in human hepatocytes (AC 50 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].
体内活性	For ICA-105665 (PF-04895162), dose-dependent alanine aminotransferase (ALT) elevations were observed in a 7-day rat toxicity study which is potentially indicative of liver toxicity. However, no histological evidence of liver injury was identified, and ALT elevations were not confirmed in a repeat 7-day study. Moreover, 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].

别名	PF-04895162
分子量	355.34
分子式	C19H15F2N3O2
CAS No.	2694728-63-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

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.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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