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

ICA-105665  (Synonyms: PF-04895162)

Cat. No.: HY-125469 Purity: 99.75%
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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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ICA-105665 Chemical Structure

ICA-105665 Chemical Structure

CAS No. : 2694728-63-5

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

ICA-105665 Related Antibodies

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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 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]
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].

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

ICA-105665 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

355.34

Formula

C19H15F2N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NN1C(C2CC2)=NC3=C(C=CC(F)=C3)C1=O)CC4=CC=C(F)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
References

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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ICA-105665 Related Classifications

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.

Keywords:

ICA-1056652694728-63-5PF-04895162ICA105665ICA 105665PF04895162PF 04895162Potassium ChannelKcsAAntiepilepticmitochondrialBSEPtransaminasebileacidsneuronalKv7KCNQ2/3KCNQ3/5BBBInhibitorinhibitorinhibit

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