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

ICA-105665  (Synonyms: PF-04895162)

目录号: HY-125469 纯度: 99.75%
COA 产品使用指南

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。

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ICA-105665 Chemical Structure

ICA-105665 Chemical Structure

CAS No. : 2694728-63-5

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2200
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1 mg ¥909
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5 mg ¥2000
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10 mg ¥3500
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25 mg ¥6500
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50 mg ¥9500
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200 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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]

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 (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 mg/kg[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

355.34

Formula

C19H15F2N3O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 250 mg/mL (703.55 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8142 mL 14.0710 mL 28.1421 mL
5 mM 0.5628 mL 2.8142 mL 5.6284 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8142 mL 14.0710 mL 28.1421 mL 70.3552 mL
5 mM 0.5628 mL 2.8142 mL 5.6284 mL 14.0710 mL
10 mM 0.2814 mL 1.4071 mL 2.8142 mL 7.0355 mL
15 mM 0.1876 mL 0.9381 mL 1.8761 mL 4.6903 mL
20 mM 0.1407 mL 0.7036 mL 1.4071 mL 3.5178 mL
25 mM 0.1126 mL 0.5628 mL 1.1257 mL 2.8142 mL
30 mM 0.0938 mL 0.4690 mL 0.9381 mL 2.3452 mL
40 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7589 mL
50 mM 0.0563 mL 0.2814 mL 0.5628 mL 1.4071 mL
60 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1726 mL
80 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8794 mL
100 mM 0.0281 mL 0.1407 mL 0.2814 mL 0.7036 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
ICA-105665
目录号:
HY-125469
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