PF 05089771

TargetMol
Product Code: TAR-T7502L
Supplier: TargetMol
CodeSizePrice
TAR-T7502L-50mg50mgEnquire
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TAR-T7502L-1mg1mg£120.00
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TAR-T7502L-5mg5mg£189.00
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TAR-T7502L-1mL1 mL * 10 mM (in DMSO)£205.00
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TAR-T7502L-10mg10mg£228.00
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TAR-T7502L-25mg25mg£332.00
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Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

1 / 1

Further Information

Bioactivity:
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.
CAS:
1235403-62-9
Formula:
C18H12Cl2FN5O3S2
Molecular Weight:
500.34
Pathway:
Membrane transporter/Ion channel
Purity:
0.9942
SMILES:
Nc1n[nH]cc1-c1cc(Cl)ccc1Oc1cc(F)c(cc1Cl)S(=O)(=O)Nc1cscn1
Target:
Sodium Channel

References

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. 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. 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. 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.