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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
Nav1.8
Available Sizes
Frequently Asked Questions
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