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PF 05089771

Catalog No. T7502L   CAS 1235403-62-9
Synonyms: PF-05089771, PF05089771

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.

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PF 05089771 Chemical Structure
PF 05089771, CAS 1235403-62-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 62.00
5 mg In stock $ 148.00
10 mg In stock $ 196.00
25 mg In stock $ 326.00
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1 mL * 10 mM (in DMSO) In stock $ 167.00
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Purity: 99.42%
Purity: 99.03%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.
Targets&IC50 CynNav1.7:12 nM (IC50), Nav1.7 (rat):171 nM (IC50), Nav1.7 (dog):13 nM (IC50), Nav1.7 (human):11 nM (IC50), Nav1.7 (mouse):8 nM (IC50)
Synonyms PF-05089771, PF05089771
Molecular Weight 500.35
Formula C18H12Cl2FN5O3S2
CAS No. 1235403-62-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL (59.96 mM)

TargetMolReferences and Literature

1. Theile JW, Fuller MD, Chapman ML. 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. PubMed PMID: 27587537. 2. Alexandrou AJ, Brown AR, Chapman ML, Estacion M, Turner J, Mis MA, Wilbrey A, Payne EC, Gutteridge A, Cox PJ, Doyle R, Printzenhoff D, Lin Z, Marron BE, West C, Swain NA, Storer RI, Stupple PA, Castle NA, Hounshell JA, Rivara M, Randall A, Dib-Hajj SD, Krafte D, Waxman SG, Patel MK, Butt RP, Stevens EB. 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. doi: 10.1371/journal.pone.0152405. PubMed PMID: 27050761; PubMed Central PMCID: PMC4822888. 3. Jones HM, Butt RP, Webster RW, Gurrell I, Dzygiel P, Flanagan N, Fraier D, Hay T, Iavarone LE, Luckwell J, Pearce H, Phipps A, Segelbacher J, Speed B, Beaumont K. Clinical Micro-Dose Studies to Explore the Human Pharmacokinetics of Four Selective Inhibitors of Human Nav1.7 Voltage-Dependent Sodium Channels. Clin Pharmacokinet. 2016 Jul;55(7):875-87. doi: 10.1007/s40262-015-0365-0. PubMed PMID: 26895021. 4. Tang Z, Chen Z, Tang B, Jiang H. Primary erythromelalgia: a review. Orphanet J Rare Dis. 2015 Sep 30;10:127. doi: 10.1186/s13023-015-0347-1. Review. PubMed PMID: 26419464; PubMed Central PMCID: PMC4589109.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Clinical Compound Library Ion Channel Inhibitor Library Bioactive Compound Library Anti-Cancer Compound Library Clinical Compound Library Bioactive Compounds Library Max ReFRAME Related Library

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Keywords

PF 05089771 1235403-62-9 Membrane transporter/Ion channel Sodium Channel Na+ channels diabetic inhibit Inhibitor neuropathy Na channels TTX-R pain tetrodotoxin PF-05089771 PF05089771 inhibitor

 

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