| Identification | Back Directory | [Name]
4-(2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide
Molecular Weight: 500.35 | [CAS]
1235403-62-9 | [Synonyms]
CS-2129
PF5089771
Nav1.7-IN-1
PF 05089771
PF-05089771 free base
PF 05089771;PF-05089771;PF05089771
4-(2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide
Benzenesulfonamide, 4-[2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolyl-
4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide
4-(2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide
Molecular Weight: 500.35 | [Molecular Formula]
C18H12Cl2FN5O3S2 | [MDL Number]
MFCD28900736 | [MOL File]
1235403-62-9.mol | [Molecular Weight]
500.35 |
| Chemical Properties | Back Directory | [Boiling point ]
699.5±65.0 °C(Predicted) | [density ]
1.673±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (>25 mg/ml) | [form ]
solid | [pka]
5.58±0.40(Predicted) | [color ]
White | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
PF-05089771 (1235403-62-9) is a potent and selective inhibitor of the voltage gated sodium channel 1.7 (Nav1.7).1,3? It is a state-dependent inhibitor with IC50 = 11 nM for the half-inactivated channels and IC50 ~ 10 μM for resting channels.1? Equipotent for human, monkey, dog, and mouse channels but 15x less potent for rat channels. Interacts equally with fast and slow inactivated Nav1.7 channels.2 | [Uses]
PF 05089771 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]. | [IC 50]
Nav1.7 | [References]
Alexandrou et al. (2016), ?Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release; PLoS One, 11 e0152405
Theile et al. (2016), The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels; Mol. Pharmacol., 90 540
Swain et al. (2017), 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; J. Med. Chem., 60 7029 |
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