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
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
N-Bromosuccinimide Price
- Product number
- PZ0311
- Product name
- PF-05089771
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $105
- Updated
- 2023/06/20
- Product number
- PZ0311
- Product name
- PF-05089771
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $424
- Updated
- 2023/06/20
- Product number
- 24449
- Product name
- PF-05089771 (tosylate)
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $98
- Updated
- 2024/03/01
- Product number
- 24449
- Product name
- PF-05089771 (tosylate)
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $186
- Updated
- 2024/03/01
- Product number
- 24449
- Product name
- PF-05089771 (tosylate)
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $389
- Updated
- 2024/03/01
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.
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