PF-05089771 (tosylate)

 化学構造式
1430806-04-4
CAS番号.
1430806-04-4
化学名:
别名:
英語名:
PF-05089771 (tosylate)
英語别名:
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
化学式:
C25H20Cl2FN5O6S3
分子量:
672.5556032
MOL File:
1430806-04-4.mol

PF-05089771 (tosylate) 物理性質

貯蔵温度 :
room temp
溶解性:
DMF: 33 mg/ml; DMSO: 33 mg/ml; DMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml
外見 :
色:
白からベージュ

安全性情報

PF-05089771 (tosylate) 価格 もっと(4)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01TOC5931
PF 05089771
1430806-04-4 10mg ¥62000 2024-03-01 購入
富士フイルム和光純薬株式会社(wako) W01TOC5931
PF 05089771
1430806-04-4 50mg ¥258000 2024-03-01 購入
Sigma-Aldrich Japan PZ0311 ≥98% (HPLC)
PF-05089771 ≥98% (HPLC)
1430806-04-4 5mg ¥22400 2024-03-01 購入
Sigma-Aldrich Japan PZ0311 ≥98% (HPLC)
PF-05089771 ≥98% (HPLC)
1430806-04-4 25mg ¥57600 2024-03-01 購入

PF-05089771 (tosylate) 化学特性,用途語,生産方法

説明

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) 上流と下流の製品情報

原材料

準備製品


PF-05089771 (tosylate) 生産企業

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