Basic information Safety Supplier Related

PF-05089771 (tosylate)

Basic information Safety Supplier Related

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
  • 4-[2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolyl-4-benzenesulfonamide, monomethylbenzenesulfonate
CAS:
1430806-04-4
MF:
C25H20Cl2FN5O6S3
MW:
672.5556032
Mol File:
1430806-04-4.mol
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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
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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)Supplier

Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Email
info@efebio.com
Beijing Solarbio Science & Tecnology Co., Ltd.
Tel
010-50973130 4009686088
Email
3193328036@qq.com
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Email
sales@invivochem.cn
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