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PF-05089771 (tosylate)

Product Name
PF-05089771 (tosylate)
CAS No.
1430806-04-4
Chemical Name
PF-05089771 (tosylate)
Synonyms
PF0508977;PF-05089771 (tosylate);PF-05089771 >=98% (HPLC);4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolylbenzenesulfonamide tosylate;4-[2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolyl-4-benzenesulfonamide, monomethylbenzenesulfonate;PF 05089771 tosylate,TTX-R,pain,Na channels,PF-05089771,neuropathy,diabetic,Sodium Channel,PF05089771,inhibit,PF 05089771,tetrodotoxin,Na+ channels,Inhibitor
CBNumber
CB54666201
Molecular Formula
C25H20Cl2FN5O6S3
Formula Weight
672.5556032
MOL File
1430806-04-4.mol
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PF-05089771 (tosylate) Property

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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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0311
Product name
PF-05089771
Purity
≥98% (HPLC)
Packaging
5MG
Price
$111
Updated
2025/07/31
Sigma-Aldrich
Product number
PZ0311
Product name
PF-05089771
Purity
≥98% (HPLC)
Packaging
25MG
Price
$447
Updated
2025/07/31
Cayman Chemical
Product number
24449
Product name
PF-05089771 (tosylate)
Purity
≥98%
Packaging
5mg
Price
$98
Updated
2024/03/01
Cayman Chemical
Product number
24449
Product name
PF-05089771 (tosylate)
Purity
≥98%
Packaging
10mg
Price
$186
Updated
2024/03/01
Cayman Chemical
Product number
24449
Product name
PF-05089771 (tosylate)
Purity
≥98%
Packaging
25mg
Price
$389
Updated
2024/03/01
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PF-05089771 (tosylate) Chemical Properties,Usage,Production

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.

Uses

PF 05089771 tosylate 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].

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

References

[1] Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405. DOI:10.1371/journal.pone.0152405
[2] Theile JW, et al. The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels. Mol Pharmacol. 2016 Nov;90(5):540-548. DOI:10.1124/mol.116.105437

PF-05089771 (tosylate) Preparation Products And Raw materials

Raw materials

Preparation Products

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PF-05089771 (tosylate) Suppliers

China 25 United Kingdom 1 United States 5 USA 1 Global 32
Sigma-Aldrich
Tel
021-61415566 800-8193336
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orderCN@merckgroup.com
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China
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Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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021-65675885
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info@efebio.com
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China
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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QQ:3008007432
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3008007409@qq.com
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China
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Beijing Solarbio Science & Tecnology Co., Ltd.
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010-50973130 18101056239
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3193328036@qq.com
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China
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TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
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32435
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InvivoChem
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+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
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United States
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HANGZHOU CLAP TECHNOLOGY CO.,LTD
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86-571-88216897,88216896 13588875226
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86-571-88216895
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sales@hzclap.com
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CHINA
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ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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18818260767
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QQ 3610331285
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sales@chemegen.com
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China
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Energy Chemical
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021-58432009 400-005-6266
Fax
021-58436166
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marketing@energy-chemical.com
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China
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Hebei Weite Medical Technology Co., Ltd
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13180081292 13180081292
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contact@wetogethermed.com
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China
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  • 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
  • 1430806-04-4