ICA-105665
Based on 1 Customer Validation
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.
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- Pureté: 99.85%
- CAS No.: 2694728-63-5
- Formule: C19H15F2N3O2
- Masse moléculaire:355.34
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2694728-63-5
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Appearance Solid
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Masse moléculaire 355.34
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Formule C19H15F2N3O2
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Color White to off-white
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SMILES
O=C(NN1C(C2CC2)=NC3=C(C=CC(F)=C3)C1=O)CC4=CC=C(F)C=C4
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Synonyms
PF-04895162
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 250 mg/mL (703.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 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 |
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