PF-05089771 (tosylate)

PF-05089771 (tosylate) 구조식 이미지
카스 번호:
1430806-04-4
상품명:
PF-05089771 (tosylate)
동의어(영문):
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
분자식:
C25H20Cl2FN5O6S3
포뮬러 무게:
672.5556032
MOL 파일:
1430806-04-4.mol
MSDS 파일:
SDS

PF-05089771 (tosylate) 속성

저장 조건
room temp
용해도
DMF: 33 mg/ml; DMSO: 33 mg/ml; DMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml
물리적 상태
가루
색상
흰색에서 베이지색

안전

PF-05089771 (tosylate) C화학적 특성, 용도, 생산

개요

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) 준비 용품 및 원자재

원자재

준비 용품


PF-05089771 (tosylate) 공급 업체

글로벌( 23)공급 업체
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Sigma-Aldrich 021-61415566 800-8193336
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