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 |
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]. | ||||||||||||||||
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]. | ||||||||||||||||
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 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(703.55 mM;Need ultrasonic) 配制储备液
* 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。 |