所有图片(1)
4-[2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolyl-benzenesulfonamide 4-methylbenzenesulfonate (1:1), 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chloro-phenoxy]-5-chloro-2-fluoro-N-thiazol-4-yl-benzenesulfonamide p-toluene sulfonate salt, PF-05089771 p-toluene sulfonate salt
C18H12Cl2FN5O3S2 · C7H8O3S
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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 30 mg/mL, clear
储存温度
room temp
SMILES字符串
ClC1=CC(C2=C(N)NN=C2)=C(OC3=C(Cl)C=C(S(NC4=CSC=N4)(=O)=O)C(F)=C3)C=C1.CC5=CC=C(S(=O)(O)=O)C=C5
InChI
1S/C18H12Cl2FN5O3S2.C7H8O3S/c19-9-1-2-14(10(3-9)11-6-24-25-18(11)22)29-15-5-13(21)16(4-12(15)20)31(27,28)26-17-7-30-8-23-17;1-6-2-4-7(5-3-6)11(8,9)10/h1-8,26H,(H3,22,24,25);2-5H,1H3,(H,8,9,10)
InChI key
NVKBPDYKPNYMDR-UHFFFAOYSA-N
生化/生理作用
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.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
PloS one, 11(4), e0152405-e0152405 (2016-04-07)
Human genetic studies show that the voltage gated sodium channel 1.7 (Nav1.7) is a key molecular determinant of pain sensation. However, defining the Nav1.7 contribution to nociceptive signalling has been hampered by a lack of selective inhibitors. Here we report
Molecular pharmacology, 97(6), 377-383 (2020-03-21)
PF-05089771 is an aryl sulfonamide Nav1.7 channel blocker that binds to the inactivated state of Nav1.7 channels with high affinity but binds only weakly to channels in the resting state. Such aryl sulfonamide Nav1.7 channel blockers bind to the extracellular
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