PF 05089771 tosylate
Based on 4 publication(s) in Google Scholar
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.
- CAS No.: 1430806-04-4
- Formula: C25H20Cl2FN5O6S3
- Molecular Weight:672.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) PF 05089771 tosylate
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Biological Activity
Description
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1430806-04-4
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Molecular Weight 672.56
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Formula C25H20Cl2FN5O6S3
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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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
PF 05089771 tosylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Feb 10;17(1):2559. [Abstract]
Influence of PF-05089771 (PF-771), tetrodotoxin (TTX), lidocaine (LIDO), carbamazepine (CBZ), and lamotrigine (LTG) on ATX-induced membrane depolarization in HEK-293 cells stably expressing hNav1.7 (hNav1.7-HEK-293).
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Nat Commun
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
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF 05089771 tosylate Related Classifications
HY-12883B Related Classifications
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