PF 05089771

Cat. No.: HY-12883 Purity: 99.87%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

PF 05089771 Chemical Structure

CAS No. : 1235403-62-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 204	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 204	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 185	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 395	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 610	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 965	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of PF 05089771:

PF 05089771 tosylate Get quote

3 Publications Citing Use of MCE PF 05089771

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View All Sodium Channel Isoform Specific Products:

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Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Nav1.7

Cellular Effect

Cell Line	Type	Value	Description	References
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	> 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	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 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	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 NaV1.1/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]
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]

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.

Clinical Trial

Molecular Weight

500.35

Formula

C₁₈H₁₂Cl₂FN₅O₃S₂

CAS No.

1235403-62-9

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (254 KB) HNMR (297 KB) RP-HPLC (257 KB) LCMS (116 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

PF 05089771 Related Classifications

Neurological Disease

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:

PF 050897711235403-62-9PF05089771PF-05089771Sodium ChannelNa channelsNa+ channelspaindiabeticneuropathytetrodotoxinTTX-RInhibitorinhibitorinhibit

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PF 05089771

Customer Review

Other Forms of PF 05089771:

PF 05089771 Related Antibodies

3 Publications Citing Use of MCE PF 05089771

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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View All Sodium Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

PF 05089771 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PF 05089771 Related Classifications

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