PF-05089771 (tosylate) 是一种有效的、具有口服活性和选择性的芳基磺酰胺 Nav1.7 抑制剂，对 hNav1.7、cynNav1.7、dogNav1.7 的 IC50 值为 11 nM、12 nM、13 nM、171 nM 和 8 nM 、ratNav1.7 和 musNav1.7。
| Cas No. | 1430806-04-4 |
| 化学名 | 4-[2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolyl-4-benzenesulfonamide, monomethylbenzenesulfonate |
| Canonical SMILES | ClC1=C(OC2=CC=C(Cl)C=C2C3=CNN=C3N)C=C(F)C(S(NC4=CSC=N4)(=O)=O)=C1.CC5=CC=C(S(O)(=O)=O)C=C5 |
| 分子式 | C18H12Cl2FN5O3S2.C7H8O3S |
| 分子量 | 672.6 |
| 溶解度 | DMSO : ≥ 34 mg/mL (67.95 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. |
