| Identification | Back Directory | [Name]
PF-05089771 (tosylate) | [CAS]
1430806-04-4 | [Synonyms]
PF-05089771 (tosylate)
PF-05089771 >=98% (HPLC)
4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate | [Molecular Formula]
C25H20Cl2FN5O6S3 | [MDL Number]
MFCD30146405 | [MOL File]
1430806-04-4.mol | [Molecular Weight]
672.556 |
| Chemical Properties | Back Directory | [storage temp. ]
room temp | [solubility ]
DMF: 33 mg/ml; DMSO: 33 mg/ml; DMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml | [form ]
powder | [color ]
white to beige | [InChIKey]
NVKBPDYKPNYMDR-UHFFFAOYSA-N | [SMILES]
ClC1=CC(C2=C(N)NN=C2)=C(OC3=C(Cl)C=C(S(NC4=CSC=N4)(=O)=O)C(F)=C3)C=C1.CC5=CC=C(S(=O)(O)=O)C=C5 |
| Hazard Information | Back Directory | [Description]
PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50s = 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50s = 0.11-25 μM), L-type calcium, and KvLQT and hERG potassium channels (IC50s = ≥10 μM), as well as human and cynomolgus monkey TRPV1 receptors (IC50s = 10 and 20 μM, respectively). PF-05089771 is also 1,000-fold selective for half-inactivated over resting Nav1.7 channels, and mutation of the domain IV voltage-sensor domain (VSD4) reduces PF-05089771 potency by approximately 100-fold. | [Uses]
PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy[1][2]. | [Biochem/physiol Actions]
PF-05089771 is a selective and potent inhibitor of the human voltage-gated sodium ion channel Nav1.7 with an IC50 value of 11 nM. PF-05089771 targets the voltage-sensing domain, preferentially interacting with, and stabilizing, inactivated channel conformations by interaction with the voltage-sensor domain (VSD) of Domain 4. Nav1.7 is expressed in sensory neurons and is critical for pain processing. PF-05089771 is being investigated for the treatment of chronic neuropathic pain. | [storage]
Desiccate at RT | [References]
[1] Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405. DOI:10.1371/journal.pone.0152405
[2] Theile JW, et al. The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels. Mol Pharmacol. 2016 Nov;90(5):540-548. DOI:10.1124/mol.116.105437 |
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