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ICA-105665

Catalog No. T11606 CAS 2694728-63-5

Synonyms: PF-04895162

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].

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ICA-105665, CAS 2694728-63-5

Pack Size	Availability	Price/USD	Quantity
100 mg	10-14 weeks	$ 1,240.00
200 mg	10-14 weeks	$ 1,878.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	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].
In vitro	ICA-105665 (PF-04895162) shows minimal cytotoxic effects in THLE and HepG2 cell lines, with IC 50 values of approximately 192 μM and 130 μM after 72 hours, respectively, and exhibits negligible cell loss in human hepatocytes, with an AC 50 of over 125 μM as determined by three assessments across two hepatocyte batches (LBN and HU4165) [1]. Furthermore, it impairs mitochondrial respiratory capacity in human hepatocytes at concentrations exceeding 11 μM when exposed for 25 minutes [1].
In vivo	ICA-105665 (PF-04895162) exhibited dose-dependent alanine aminotransferase (ALT) elevations in a 7-day rat toxicity study, suggesting potential liver toxicity. Nonetheless, no histological liver injury was observed, and subsequent 7-day studies did not confirm ALT elevations. Further, both 28-day and 6-month rat studies, as well as up to 9-month toxicity studies in cynomolgus monkeys, showed no transaminase elevations or liver toxicity. Additionally, ICA-105665 (PF-04895162) has shown broad-spectrum antiseizure efficacy across several animal models, including maximal electroshock, 6 Hz seizures, pentylenetetrazole, and electrical kindling, at doses ranging from <1 to 5 mg/kg [3].

Synonyms	PF-04895162
Molecular Weight	355.34
Formula	C19H15F2N3O2
CAS No.	2694728-63-5

Storage

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

References and Literature

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.

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Keywords

ICA-105665 2694728-63-5 Others PF 04895162 ICA 105665 PF04895162 PF-04895162 ICA105665 inhibitor inhibit

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