1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. PF 05089771

PF 05089771 

Cat. No.: HY-12883 Purity: 99.32%
Handling Instructions

PF 05089771 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, 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

PF 05089771 Chemical Structure

CAS No. : 1235403-62-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of PF 05089771:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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Description

PF 05089771 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy[1][2].

IC50 & Target

IC50: 11 nM (hNav1.7), 12 nM (cynNav1.7), 13 nM (dogNav1.7), 171 nM (ratNav1.7), 8 nM (musNav1.7)[1][2].

In Vitro

PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4)[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].

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

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 34 mg/mL (67.95 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

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

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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.32%

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Keywords:

PF 05089771PF05089771PF-05089771Sodium ChannelNa channelsNa+ channelspaindiabeticneuropathytetrodotoxinTTX-RInhibitorinhibitorinhibit

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PF 05089771
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HY-12883
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