PF 04531083

PF 04531083 is an orally active and selective NaV1.8 blocker with an IC50 of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain[1][2][3].

Product Specifications

CAS Number

[1079400-07-9]

UNSPSC

12352005

Hazard Statement

H302

Target

Sodium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/PF_04531083.html

Purity

98.33

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

ClC1=CC=C(OC)C=C1C2=C(N=C(NC(C3=CC=NN3C)=O)C=C2)N

Molecular Formula

C17H16ClN5O2

Molecular Weight

357.79

Precautions

H302

References & Citations

[1]Yekkirala AS, et al. Breaking barriers to novel analgesic drug development. Nat Rev Drug Discov. 2017 Aug;16 (8) :545-564. |[2]Bagal SK, et al. Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain. ACS Med Chem Lett. 2015 Apr 29;6 (6) :650-4.|[3]Cleary CM, et al. Disordered breathing in a Pitt-Hopkins syndrome model involves Phox2b-expressing parafacial neurons and aberrant Nav1.8 expression. Nat Commun. 2021 Oct 13;12 (1) :5962.