Art. -Nr.: HY-12883

PF 05089771

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

PF 05089771 is a potent, orally active and selective arylsulfonamide Na_v1.7 inhibitor, with IC₅₀ values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNa_v1.7, cynNa_v1.7, dogNa_v1.7, ratNa_v1.7, and musNa_v1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.

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Reinheit: 99.87%
CAS. Nr.: 1235403-62-9
Formel: C₁₈H₁₂Cl₂FN₅O₃S₂
Molecular Weight:500.35

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PF 05089771 Chemical Structure

CAS. Nr.: 1235403-62-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Nav1.7

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	11 nM Compound: 1b; PF-05089771	Inhibition of human Nav1.7 expressed in HEK293 cells Inhibition of human Nav1.7 expressed in HEK293 cells	[PMID: 28389149]
HEK293	IC₅₀	25 μM Compound: 1b; PF-05089771	Inhibition of human Nav1.5 expressed in HEK293 cells Inhibition of human Nav1.5 expressed in HEK293 cells	[PMID: 28389149]
HEK293	IC₅₀	>10 μM Compound: 1a; PF-05089771	Inhibition of 50% inactivated human Nav1.7alpha expressed in HEK293 cells measured after 5 to 10 mins post compound washout by PatchXpress automated electrophysiology method Inhibition of 50% inactivated human Nav1.7alpha expressed in HEK293 cells measured after 5 to 10 mins post compound washout by PatchXpress automated electrophysiology method	[PMID: 28465103]
HEK293	IC₅₀	11 nM Compound: 1a; PF-05089771	Inhibition of 50% inactivated human Nav1.5alpha expressed in HEK293 cells measured after 5 to 10 mins post compound washout by PatchXpress automated electrophysiology method Inhibition of 50% inactivated human Nav1.5alpha expressed in HEK293 cells measured after 5 to 10 mins post compound washout by PatchXpress automated electrophysiology method	[PMID: 28465103]
HEK293	IC₅₀	>10 μM Compound: 3; PF-05089771	Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.8 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	0.011 μM Compound: 3; PF-05089771	Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.7 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	0.11 μM Compound: 3; PF-05089771	Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.2 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	0.16 μM Compound: 3; PF-05089771	Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.6 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	0.85 μM Compound: 3; PF-05089771	Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.1 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	10 μM Compound: 3; PF-05089771	Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.4 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	11 μM Compound: 3; PF-05089771	Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.3 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	25 μM Compound: 3; PF-05089771	Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay Inhibition of human Nav1.5 expressed in HEK293 cells by electrophysiology assay	[PMID: 31012583]
HEK293	IC₅₀	3.5 μM Compound: 9; PF-05089771	Inhibition of URAT1 (unknown origin) expressed in HEK293 cells assessed as suppression of [14C]-uric acid uptake preincubated for 15 mins followed by [14C]-uric acid addition measured after 2 mins by liquid scintillation counting Inhibition of URAT1 (unknown origin) expressed in HEK293 cells assessed as suppression of [14C]-uric acid uptake preincubated for 15 mins followed by [14C]-uric acid addition measured after 2 mins by liquid scintillation counting	10.1039/C6MD00190D
HEK293-A	IC₅₀	>100000 nM Compound: II	Inhibition of human NaV1.5/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method Inhibition of human NaV1.5/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method	[PMID: 32392056]
HEK293-A	IC₅₀	13 nM Compound: II	Inhibition of human NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method Inhibition of human NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method	[PMID: 32392056]
HEK293-A	IC₅₀	4.9 nM Compound: II	Inhibition of mouse NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method Inhibition of mouse NaV1.7/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method	[PMID: 32392056]
HEK293-A	IC₅₀	>100000 nM Compound: II	Inhibition of human NaV1.1/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method Inhibition of human NaV1.1/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method	[PMID: 32392056]

In Vitro

PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Na_v1.5 and Na_v1.8 channels (IC₅₀s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Na_v1.2 to 900-fold for Na_v1.3 and Na_v1.4)^[1].
PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5, Fig 5D) whilst 100 nM resulted in complete block^[1].

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

Chemical Information

CAS. Nr. 1235403-62-9
Appearance Solid
Molecular Weight 500.35
Formel C₁₈H₁₂Cl₂FN₅O₃S₂
Color White to off-white
SMILES

O=S(C1=CC(Cl)=C(OC2=CC=C(Cl)C=C2C3=CNN=C3N)C=C1F)(NC4=CSC=N4)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Nat Commun

Molecular determinant of low-voltage dependence of human Nav1.7 inactivation revealed by efficacy-based Nav1.7 selective inhibitor. [Abstract]

2026 Feb 10;17(1):2559. PMID: 41667447
Nat Commun

Structural mapping of Nav1.7 antagonists. [Abstract]

2023 Jun 3;14(1):3224. PMID: 37270609
Front Pharmacol

Mechanisms Underlying Gastrodin Alleviating Vincristine-Induced Peripheral Neuropathic Pain. [Abstract]

2021 Dec 16:12:744663. PMID: 34975470
FEBS J

Transcription factor mesenchyme homeobox protein 2 (MEOX2) modulates nociceptor function. [Abstract]

2022 Jun;289(12):3457-3476. PMID: 35029322

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (199.86 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

1.9986 mL

9.9930 mL

19.9860 mL

5 mM

0.3997 mL

1.9986 mL

3.9972 mL

10 mM

0.1999 mL

0.9993 mL

1.9986 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.00 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

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

Solubility: ≥ 2.25 mg/mL (4.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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 3

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

Solubility: ≥ 2.25 mg/mL (4.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 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 (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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% Tween-80 in Saline

Solubility: 5 mg/mL (9.99 mM); Suspended solution; Need ultrasonic

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 (278 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]. Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405. [Content Brief]

[2]. Theile JW, et al. The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels. Mol Pharmacol. 2016 Nov;90(5):540-548. [Content Brief]

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9986 mL	9.9930 mL	19.9860 mL	49.9650 mL
	5 mM	0.3997 mL	1.9986 mL	3.9972 mL	9.9930 mL
	10 mM	0.1999 mL	0.9993 mL	1.9986 mL	4.9965 mL
	15 mM	0.1332 mL	0.6662 mL	1.3324 mL	3.3310 mL
	20 mM	0.0999 mL	0.4997 mL	0.9993 mL	2.4983 mL
	25 mM	0.0799 mL	0.3997 mL	0.7994 mL	1.9986 mL
	30 mM	0.0666 mL	0.3331 mL	0.6662 mL	1.6655 mL
	40 mM	0.0500 mL	0.2498 mL	0.4997 mL	1.2491 mL
	50 mM	0.0400 mL	0.1999 mL	0.3997 mL	0.9993 mL
	60 mM	0.0333 mL	0.1666 mL	0.3331 mL	0.8328 mL
	80 mM	0.0250 mL	0.1249 mL	0.2498 mL	0.6246 mL
	100 mM	0.0200 mL	0.0999 mL	0.1999 mL	0.4997 mL

Keywords

PF 05089771

4 Cited Publications

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PF 05089771

Membrane Transporter/Ion Channel Compound Library

Anti-diabetic Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Targeted Diversity Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PF 05089771

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF 05089771

Membrane Transporter/Ion Channel Compound Library

Anti-diabetic Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Targeted Diversity Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) PF 05089771

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF 05089771 Related Classifications

Art. -Nr.: HY-12883