PF-05089771 (tosylate)

PF-05089771 (tosylate) Structure
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;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
Molecular Weight:
672.5556032
MOL File:
1430806-04-4.mol
MSDS File:
SDS
Modify Date:
2023/9/4 15:50:00

PF-05089771 (tosylate) 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) Chemical Properties,Uses,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.

PF-05089771 (tosylate) Preparation Products And Raw materials

Raw materials

Preparation Products

PF-05089771 (tosylate) Suppliers

Global( 22)Suppliers
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Cayman Chemical Company (800) 364-9897 United States 6618 81 Inquiry
Shanghai EFE Biological Technology Co., Ltd. 021-65675885 18964387627 China 9707 58 Inquiry
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PF-05089771 (tosylate) Spectrum

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 1430806-04-4