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
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PF 05089771 tosylate
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Biological Activity
IC50: 11 nM (hNav1.7), 12 nM (cynNav1.7), 13 nM (dogNav1.7), 171 nM (ratNav1.7), 8 nM (musNav1.7)[1][2].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| 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 -
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
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)
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