PF 05089771

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Cat.No. 5931 - PF 05089771 | C18H12Cl2FN5O3S2.C7H8O3S | CAS No. 1430806-04-4
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 (1)
Reviews (1)
Literature (5)

Biological Activity

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

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

Technical Data

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

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

Preparing Stock Solutions

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

1 Citation for PF 05089771

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

Cheng et al (2019) The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes. Theranostics 9 4287 PMID: 31285762


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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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Literature in this Area

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