Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H12Cl2FN5O3S2.C7H8O3S |
| Molecular Weight | 672.556 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC=C(C=C1)S(O)(=O)=O.NC2=C(C=NN2)C3=CC(Cl)=CC=C3OC4=CC(F)=C(C=C4Cl)S(=O)(=O)NC5=CSC=N5
InChI
InChIKey=NVKBPDYKPNYMDR-UHFFFAOYSA-N
InChI=1S/C18H12Cl2FN5O3S2.C7H8O3S/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;1-6-2-4-7(5-3-6)11(8,9)10/h1-8,26H,(H3,22,24,25);2-5H,1H3,(H,8,9,10)
| Molecular Formula | C7H8O3S |
| Molecular Weight | 172.202 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | C18H12Cl2FN5O3S2 |
| Molecular Weight | 500.354 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
PF-05089771 is an oral administrated Nav1.7 channel inhibitor. PF-05089771 provided the best opportunity to explore Nav1.7 blockade for the treatment of acute or chronic pain conditions. PF-05089771 has completed Phase II clinical trials of third molar extraction and primary inherited erythromelalgia. The magnitude of efficacy of PF-05089771 in the randomized, placebo-controlled, double-blind clinical study in subjects with painful diabetic peripheral neuropathy was disappointing. Although there was a trend towards a reduction in pain and improvement in sleep rating in patients with painful DPN when compared to placebo treatment, this was not statistically significant.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Recent progress in sodium channel modulators for pain. | 2014 Aug 15 |
|
| Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. | 2016 |
|
| Pharmacological reversal of a pain phenotype in iPSC-derived sensory neurons and patients with inherited erythromelalgia. | 2016 Apr 20 |
|
| Clinical Micro-Dose Studies to Explore the Human Pharmacokinetics of Four Selective Inhibitors of Human Nav1.7 Voltage-Dependent Sodium Channels. | 2016 Jul |
|
| Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na(V)1.7. | 2017 Aug 24 |
|
| Efficacy of the Nav1.7 blocker PF-05089771 in a randomised, placebo-controlled, double-blind clinical study in subjects with painful diabetic peripheral neuropathy. | 2018 Aug |
|
| Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors. | 2018 Jan 23 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 01:53:44 UTC 2023
by
admin
on
Sat Dec 16 01:53:44 UTC 2023
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| Record UNII |
NG8E748OWS
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| Record Status |
Validated (UNII)
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| Record Version |
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Created by
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1430806-04-4
Created by
admin on Sat Dec 16 01:53:44 UTC 2023 , Edited by admin on Sat Dec 16 01:53:44 UTC 2023
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NG8E748OWS
Created by
admin on Sat Dec 16 01:53:44 UTC 2023 , Edited by admin on Sat Dec 16 01:53:44 UTC 2023
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