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

PF 05089771 tosylate 

Cat. No.: HY-12883B
Handling Instructions

PF 05089771 tosylate 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 tosylate Chemical Structure

PF 05089771 tosylate Chemical Structure

CAS No. : 1430806-04-4

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Description

PF 05089771 tosylate 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) whilst 100 nM resulted in complete block[1].

Molecular Weight

672.56

Formula

C₂₅H₂₀Cl₂FN₅O₆S₃

CAS No.

1430806-04-4

SMILES

O=S(C1=CC(Cl)=C(OC2=CC=C(Cl)C=C2C3=C(N)NN=C3)C=C1F)(NC4=CSC=N4)=O.CC5=CC=C(S(O)(=O)=O)C=C5

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

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

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PF 05089771 tosylate
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