PF 05089771

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Description: Potent and selective Nav1.7 channel blocker
Chemical Name: 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Reviews (1)

Biological Activity for PF 05089771

PF 05089771 is a potent and selective Nav1.7 channel blocker (IC50 = 8, 11 and 171 nM for mouse, human and rat Nav1.7, respectively). Exhibits selectivity for Nav1.7 over other Nav1 channels (IC50 values are 0.11, 0.16, 0.85, 10, 11 and 25 μM for Nav1.2, Nav1.6, Nav1.1, Nav1.4, Nav1.3 and Nav1.5, respectively). Also exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. Blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries for PF 05089771

PF 05089771 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.

Technical Data for PF 05089771

M. Wt 672.56
Formula C18H12Cl2FN5O3S2.C7H8O3S
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1430806-04-4
PubChem ID 71554187
InChI Key NVKBPDYKPNYMDR-UHFFFAOYSA-N
Smiles ClC1=C(OC2=CC=C(Cl)C=C2C3=CNN=C3N)C=C(F)C(S(NC4=CSC=N4)(=O)=O)=C1.CC5=CC=C(S(=O)(O)=O)C=C5

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PF 05089771

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 67.26 100

Preparing Stock Solutions for PF 05089771

The following data is based on the product molecular weight 672.56. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.49 mL 7.43 mL 14.87 mL
5 mM 0.3 mL 1.49 mL 2.97 mL
10 mM 0.15 mL 0.74 mL 1.49 mL
50 mM 0.03 mL 0.15 mL 0.3 mL

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Keywords: PF 05089771, PF 05089771 supplier, PF05089771, potent, selective, Nav1.7, sodium, channels, neuropathic, pain, Voltage-gated, Sodium, Channels, 5931, Tocris Bioscience

6 Citations for PF 05089771

Citations are publications that use Tocris products. Selected citations for PF 05089771 include:

Ellen A et al (2019) Tetrodotoxin-Sensitive Sodium Channels Mediate Action Potential Firing and Excitability in Menthol-Sensitive Vglut3-Lineage Sensory Neurons. J Neurosci 39 7086-7101 PMID: 31300524

Oliver et al (2023) Bringing to light the physiological and pathological firing patterns of human induced pluripotent stem cell-derived neurons using optical recordings. Front Cell Neurosci 16 1039957 PMID: 36733665

Wei et al (2023) Ectopic expression of Nav1.7 in spinal dorsal horn neurons induced by NGF contributes to neuropathic pain in a mouse spinal cord injury model. Front Mol Neurosci 16 1091096 PMID: 36937049

Darik A et al (2022) NaV1.1 is essential for proprioceptive signaling and motor behaviors. Elife 11 PMID: 36278870


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Reviews for PF 05089771

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Study of PF 05089771's Nav1.7 blocking efficacy.
By Anonymous on 12/26/2019
Species: Human

The effect of PF-05089771, a selective, peripherally restricted Nav1.7 sodium channel blocker on pain due to diabetic peripheral neuropathy was investigated.

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