PF-01247324

Name: PF-01247324
Brand: MedChemExpress
SKU: HY-101383
Rating: 4.5 (1 reviews)

Cat. No.: HY-101383 Purity: 99.63%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PF-01247324 is a selective and orally bioavailable Na_v1.8 channel blocker with an IC₅₀ of 196 nM for recombinant human Na_v1.8 channel.

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

PF-01247324 Chemical Structure

CAS No. : 875051-72-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 92	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 92	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 312	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 540	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE PF-01247324

•Front Pharmacol. 16 December 2021.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sodium Channel Isoform Specific Products:

View All Isoforms

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
Protocol
Purity & Documentation
References
Customer Review

Description

PF-01247324 is a selective and orally bioavailable Na_v1.8 channel blocker with an IC₅₀ of 196 nM for recombinant human Na_v1.8 channel.

IC₅₀ & Target

Nav1.8

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.19 μM Compound: 3	Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology	[PMID: 26101568]
HEK293	IC₅₀	12.8 μM Compound: 3	Inhibition of human Nav1.2 expressed in HEK293 cells by IonWorks Quattro selectivity assay Inhibition of human Nav1.2 expressed in HEK293 cells by IonWorks Quattro selectivity assay	[PMID: 26101568]
HEK293	IC₅₀	13 μM Compound: 3	Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay	[PMID: 26101568]
HEK293	IC₅₀	19 μM Compound: 3	Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay	[PMID: 26101568]
HEK293	IC₅₀	2.6 μM Compound: 3	Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay	[PMID: 26101568]
HEK293	IC₅₀	9 μM Compound: 3	Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay	[PMID: 26101568]
SH-SY5Y	IC₅₀	14 μM Compound: 3	Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay Inhibition of human Nav1.2 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay	[PMID: 26101568]
SH-SY5Y	IC₅₀	14 μM Compound: 3	Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay Inhibition of human Nav1.3 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay	[PMID: 26101568]
SH-SY5Y	IC₅₀	14 μM Compound: 3	Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay Inhibition of human Nav1.7 expressed in SHSY5Y cells assessed as reduction in blue fluorescent signal by VSP-FRET assay	[PMID: 26101568]

In Vitro

PF-01247324 inhibits native tetrodotoxin-resistant (TTX-R) currents in human dorsal root ganglion (DRG) neurons (IC₅₀=331 nM) and in recombinantly expressed h Na_v1.8 channels (IC₅₀=196 nM), with 50-fold selectivity over recombinantly expressed TTX-R hNav1.5 channels (IC₅₀=10 μM) and 65-100-fold selectivity over TTX-sensitive (TTX-S) channels (IC₅₀=10-18 μM). In vitro current clamp shows that PF-01247324 reduces excitability in both rat and human DRG neurons and also alters the waveform of the action potential^[1].

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

In Vivo

Experiments n rodents demonstrates efficacy in both inflammatory and neuropathic pain models. PF-01247324 reduces phase 2 flinching by 37% at 100 mg/kg. There is a significant effect of 30 mg/kg of PF-01247324 in the rat model carrageenan-induced thermal hyperalgesia and in CFA-induced mechanical hyperalgesia at exposures of 0.218 and 0.126 μM respectively^[1]. Mice that received PF-01247324 shows significant improvements in motor coordination and cerebellar-like symptoms compared to control^[2].

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

Molecular Weight

330.60

Formula

C₁₃H₁₀Cl₃N₃O

CAS No.

875051-72-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=NC(N)=C(C2=CC(Cl)=CC(Cl)=C2Cl)C=C1)NC

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 : ≥ 30 mg/mL (90.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0248 mL	15.1240 mL	30.2480 mL
5 mM	0.6050 mL	3.0248 mL	6.0496 mL
10 mM	0.3025 mL	1.5124 mL	3.0248 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.

Molarity Calculator
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 99.63%

Select Batch:

Data Sheet (276 KB) SDS (420 KB)

COA (249 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. Payne CE, et al. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. [Content Brief]

[2]. Shields SD, et al. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067. [Content Brief]

Animal Administration
^[1]^[2]

Rats: For male Sprague Dawley rats (170-300 g), PF-01247324 is formulated as solutions of 0, 10, 30, 100 mg/kg in 0.5%MC/0.1%Tween 80 vehicle and dosed via oral gavage prior to behavioural testing. Test animals are placed in a box separated by walls with a wire mesh floor allowing access to the plantar surface of the paw. Tactile testing is conducted^[1].

Mice: PF-01247324 is suspended in 0.5% methylcellulose, 0.1% Tween 80 and administered by oral gavage at a dose of 1000 mg/kg in a volume of 10 mL/kg one hour before behavioral testing. Control groups are administered an equal volume of vehicle^[2].

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

References

[1]. Payne CE, et al. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br J Pharmacol. 2015 May;172(10):2654-70. [Content Brief]

[2]. Shields SD, et al. Oral administration of PF-01247324, a subtype-selective Nav1.8 blocker, reverses cerebellar deficits in a mouse model of multiple sclerosis. PLoS One. 2015 Mar 6;10(3):e0119067. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0248 mL	15.1240 mL	30.2480 mL	75.6201 mL
	5 mM	0.6050 mL	3.0248 mL	6.0496 mL	15.1240 mL
	10 mM	0.3025 mL	1.5124 mL	3.0248 mL	7.5620 mL
	15 mM	0.2017 mL	1.0083 mL	2.0165 mL	5.0413 mL
	20 mM	0.1512 mL	0.7562 mL	1.5124 mL	3.7810 mL
	25 mM	0.1210 mL	0.6050 mL	1.2099 mL	3.0248 mL
	30 mM	0.1008 mL	0.5041 mL	1.0083 mL	2.5207 mL
	40 mM	0.0756 mL	0.3781 mL	0.7562 mL	1.8905 mL
	50 mM	0.0605 mL	0.3025 mL	0.6050 mL	1.5124 mL
	60 mM	0.0504 mL	0.2521 mL	0.5041 mL	1.2603 mL
	80 mM	0.0378 mL	0.1891 mL	0.3781 mL	0.9453 mL

PF-01247324 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-01247324875051-72-2PF01247324PF 01247324Sodium ChannelNa channelsNa+ channelsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

PF-01247324

Customer Review

PF-01247324 Related Antibodies

1 Publications Citing Use of MCE PF-01247324

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Sodium Channel Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

PF-01247324 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

PF-01247324 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report