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| | PF-05089771 (tosylate) Basic information |
| Product Name: | PF-05089771 (tosylate) | | Synonyms: | PF-05089771 (tosylate);4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate;PF-05089771 >=98% (HPLC);PF 05089771 tosylate,TTX-R,pain,Na channels,PF-05089771,neuropathy,diabetic,Sodium Channel,PF05089771,inhibit,PF 05089771,tetrodotoxin,Na+ channels,Inhibitor;PF0508977 | | CAS: | 1430806-04-4 | | MF: | C25H20Cl2FN5O6S3 | | MW: | 672.5556032 | | EINECS: | | | Product Categories: | | | Mol File: | 1430806-04-4.mol |  |
| | PF-05089771 (tosylate) Chemical Properties |
| 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 |
| | PF-05089771 (tosylate) Usage And Synthesis |
| 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. | | 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 |
| | PF-05089771 (tosylate) Preparation Products And Raw materials |
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