| Name | PF 05089771 |
|---|---|
| Supplier | Tocris Bioscience |
| Catalog | 4916 |
| Prices | $149.00, $629.00 |
| Sizes | 10 mg, 50 mg |
| Function Type | Blocker |
| Cas Number | 1430806-04-4 |
| Chemical Name | 4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamidetosylate |
| Formula | C18H12Cl2FN5O3S2.C7H8O3S |
| Molecular Weight | 672.56 |
| Purity | >98 % |
| Description | Potent and selective Na v 1.7 channel blocker (IC 50 = 8, 11 and 171 nM for mouse, human and rat Na v 1.7, respectively). Exhibits selectivity for Na v 1.7 over other Na v 1 channels (IC 50 values are 0.11, 0.16, 0.85, 10, 11 and 25 μ M for Na v 1.2, Na v 1.6, Na v 1.1, Na v 1.4, Na v 1.3 and Na v 1.5, respectively). Also exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. Blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro . |
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Venkatesan AM, Dehnhardt CM, Delos Santos E, Chen Z, Dos Santos O, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham RT, Chaudhary I, Mansour TS. J Med Chem. 2010 Mar 25;53(6):2636-45.
Mallon R, Feldberg LR, Lucas J, Chaudhary I, Dehnhardt C, Santos ED, Chen Z, dos Santos O, Ayral-Kaloustian S, Venkatesan A, Hollander I. Clin Cancer Res. 2011 May 15;17(10):3193-203.