PF-05089771

PF-05089771
Legal status
Legal status	US: Investigational New Drug;
Identifiers
	IUPAC name 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzene-1-sulfonamide;
CAS Number	1235403-62-9;
PubChem CID	46840946;
ChemSpider	29411106;
UNII	25U4N985O2;
ChEMBL	ChEMBL2325014;
CompTox Dashboard (EPA)	DTXSID301336085 ;
Chemical and physical data
Formula	C18H12Cl2FN5O3S2
Molar mass	500.34 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC(=C(C=C1Cl)C2=C(NN=C2)N)OC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=CSC=N4)F;
	InChI InChI=1S/C18H12Cl2FN5O3S2/c19-9-1-2-14(10(3-9)11-6-24-25-18(11)22)29-15-5-13(21)16(4-12(15)20)31(27,28)26-17-7-30-8-23-17/h1-8,26H,(H3,22,24,25); Key:ZYSCOUXLBXGGIM-UHFFFAOYSA-N;

PF-05089771 is a selective, small-molecule Na_v1.7 and Na_v1.8 voltage-gated sodium channel blocker under development by Pfizer as a novel analgesic.^[1]^[2]^[3] As of June 2014, it has completed phase II clinical trials for wisdom tooth removal and primary erythromelalgia.^[4]

References

^ McMahon SB, Koltzenburg M, Tracey I, Turk D (March 2013). Wall & Melzack's Textbook of Pain. Elsevier Health Sciences. p. 508. ISBN 978-0702053740.
^ Martz L (June 2014). "Nav-i-gating antibodies for pain". SciBX: Science-Business EXchange. 7 (23): 662. doi:10.1038/scibx.2014.662.
^ Alexandrou AJ, Brown AR, Chapman ML, Estacion M, Turner J, Mis MA, et al. (6 April 2016). "Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release". PLOS ONE. 11 (4): e0152405. Bibcode:2016PLoSO..1152405A. doi:10.1371/journal.pone.0152405. PMC 4822888. PMID 27050761.
^ Bagal SK, Chapman ML, Marron BE, Prime R, Storer RI, Swain NA (August 2014). "Recent progress in sodium channel modulators for pain". Bioorganic & Medicinal Chemistry Letters. 24 (16): 3690–3699. doi:10.1016/j.bmcl.2014.06.038. PMID 25060923.

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