ICA-105665
Product Specifications
Product Name Alternative
PF-04895162
UNSPSC 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 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].
Target Antigen
Potassium Channel
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/ica-105665.html
Purity
99.85
Solubility
DMSO : 250 mg/mL (ultrasonic)
Smiles
O=C(NN1C(C2CC2)=NC3=C(C=CC(F)=C3)C1=O)CC4=CC=C(F)C=C4
Molecular Weight
355.34
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-125469/ICA-105665-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-125469/ICA-105665-SDS-MedChemExpress.pdf
Clinical Information
Phase 2
CAS Number
2694728-63-5
Available Sizes
Curated Selection
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