PF-05089771 (tosylate)

PF-05089771 (tosylate) Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

PF-05089771 is a voltage-gated sodium channel 1.7 (Na_v1.7) blocker (IC₅₀s = 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Na_v1.7 splice variants, respectively). It is selective for Na_v1.7 over Na_v1.1-1.6 and 1.8 channels (IC₅₀s = 0.11-25 μM), L-type calcium, and K_vLQT 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 Na_v1.7 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) Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

PF-05089771 (tosylate) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
HANGZHOU CLAP TECHNOLOGY CO.,LTD	86-571-88216897,88216896 13588875226	sales@hzclap.com	CHINA	6313	58
InvivoChem	+1-708-310-1919 +1-13798911105	sales@invivochem.cn	United States	6393	58
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3136	58
TargetMol Chemicals Inc.	+1-781-999-5354	support@targetmol.com	United States	19973	58
Aladdin Scientific	+1-+1(833)-552-7181	sales@aladdinsci.com	United States	57511	58
Sigma-Aldrich	021-61415566 800-8193336	orderCN@merckgroup.com	China	51471	80
ATK CHEMICAL COMPANY LIMITED	3429815786 13301662590	sales@atkchemical.com	China	10059	55
Shanghai EFE Biological Technology Co., Ltd.	021-65675885 18964387627	info@efebio.com	China	9708	58
Beijing Solarbio Science & Tecnology Co., Ltd.	010-50973130 4009686088	3193328036@qq.com	China	29795	68
BOC Sciences	--	info@bocsci.com	USA	0	65

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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
• 1430806-04-4