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Tocris/PF 05089771/5931/50/50 mg

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货号: 5931/50

品牌: Tocris

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Description: Potent and selective Na_v1.7 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)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent and selective Na_v1.7 channel blocker (IC₅₀ = 8, 11 and 171 nM for mouse, human and rat Na_v1.7, respectively). Exhibits selectivity for Na_v1.7 over other Na_v1 channels (IC₅₀ values are 0.11, 0.16, 0.85, 10, 11 and 25 μM for Na_v1.2, Na_v1.6, Na_v1.1, Na_v1.4, Na_v1.3 and Na_v1.5, 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.

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Cao et al (2016) Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia. Sci.Transl.Med. 8 335ra56 PMID: 27099175

Alexandrou et al (2016) Subtype-selective small molecule inhibitors reveal a fundamental role for Na_v1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release. PLoS One 11 e0152405 PMID: 27050761

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

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