Art. -Nr.: HY-110325

PF-04885614

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PF-04885614 is a potent NaV1.8 inhibitor, extracted from patent US2018328915. PF-04885614 has potential for neurological and neurodevelopmental diseases treatment.

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Reinheit: 97.00%
CAS. Nr.: 1480833-70-2
Formel: C₁₃H₁₄F₃N₃O
Molecular Weight:285.26

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-04885614 Chemical Structure

CAS. Nr.: 1480833-70-2

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Biologische Aktivität
- Beschreibung
- Cellular Effect
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PF-04885614 is a potent NaV1.8 inhibitor, extracted from patent US2018328915. PF-04885614 has potential for neurological and neurodevelopmental diseases treatment^[1].

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.053 μM Compound: 13	Inhibition of 50% inactivated recombinant human Nav1.8 expressed in HEK293 cells coexpressing Nav beta1 subunit at holding potential of -120 mV by manual patch electrophysiology method Inhibition of 50% inactivated recombinant human Nav1.8 expressed in HEK293 cells coexpressing Nav beta1 subunit at holding potential of -120 mV by manual patch electrophysiology method	10.1039/C6MD00281A
HEK293	IC₅₀	1.8 μM Compound: 13	Inhibition of Cy3B-labeled ligand binding to recombinant human ERG expressed in HEK293 cells by fluorescence polarization method Inhibition of Cy3B-labeled ligand binding to recombinant human ERG expressed in HEK293 cells by fluorescence polarization method	10.1039/C6MD00281A
HEK293	IC₅₀	11 μM Compound: 13	Inhibition of 50% inactivated recombinant human Nav1.1 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method Inhibition of 50% inactivated recombinant human Nav1.1 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method	10.1039/C6MD00281A
HEK293	IC₅₀	16 μM Compound: 13	Inhibition of 50% inactivated recombinant human Nav1.2 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method Inhibition of 50% inactivated recombinant human Nav1.2 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method	10.1039/C6MD00281A
HEK293	IC₅₀	2.6 μM Compound: 13	Inhibition of recombinant human ERG expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method Inhibition of recombinant human ERG expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method	10.1039/C6MD00281A
HEK293	IC₅₀	27 μM Compound: 13	Inhibition of 50% inactivated recombinant human Nav1.5 expressed in HEK293 cells at holding potential of -150 mV by PatchXpress automated electrophysiology method Inhibition of 50% inactivated recombinant human Nav1.5 expressed in HEK293 cells at holding potential of -150 mV by PatchXpress automated electrophysiology method	10.1039/C6MD00281A
HEK293	IC₅₀	4.2 μM Compound: 13	Inhibition of 50% inactivated recombinant human Nav1.6 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method Inhibition of 50% inactivated recombinant human Nav1.6 expressed in HEK293 cells at holding potential of -120 mV by manual patch electrophysiology method	10.1039/C6MD00281A
HEK293	IC₅₀	7 μM Compound: 13	Inhibition of 50% inactivated recombinant human Nav1.7 expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method Inhibition of 50% inactivated recombinant human Nav1.7 expressed in HEK293 cells at holding potential of -120 mV by PatchXpress automated electrophysiology method	10.1039/C6MD00281A

Chemical Information

CAS. Nr. 1480833-70-2
Appearance Solid
Molecular Weight 285.26
Formel C₁₃H₁₄F₃N₃O
Color Off-white to light yellow
SMILES

NC(C)(C)C1=NC=C(C2=CC=C(OC(F)(F)F)C=C2)N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (876.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.5056 mL

17.5279 mL

35.0557 mL

5 mM

0.7011 mL

3.5056 mL

7.0111 mL

10 mM

0.3506 mL

1.7528 mL

3.5056 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (7.29 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Brady MAHER, et al. Treatment of Neurological and Neurodevelopmental Diseases and Disorders Associated with Aberrant Ion Channel Expression and Activity. US20180328915A1.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	3.5056 mL	17.5279 mL	35.0557 mL	87.6393 mL
	5 mM	0.7011 mL	3.5056 mL	7.0111 mL	17.5279 mL
	10 mM	0.3506 mL	1.7528 mL	3.5056 mL	8.7639 mL
	15 mM	0.2337 mL	1.1685 mL	2.3370 mL	5.8426 mL
	20 mM	0.1753 mL	0.8764 mL	1.7528 mL	4.3820 mL
	25 mM	0.1402 mL	0.7011 mL	1.4022 mL	3.5056 mL
	30 mM	0.1169 mL	0.5843 mL	1.1685 mL	2.9213 mL
	40 mM	0.0876 mL	0.4382 mL	0.8764 mL	2.1910 mL
	50 mM	0.0701 mL	0.3506 mL	0.7011 mL	1.7528 mL
	60 mM	0.0584 mL	0.2921 mL	0.5843 mL	1.4607 mL
	80 mM	0.0438 mL	0.2191 mL	0.4382 mL	1.0955 mL
	100 mM	0.0351 mL	0.1753 mL	0.3506 mL	0.8764 mL

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PF-04885614

Membrane Transporter/Ion Channel Compound Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-04885614

Membrane Transporter/Ion Channel Compound Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-04885614 Related Classifications

HY-110325 Related Classifications