PF-05089771 free base
CAS No. 1235403-62-9
PF-05089771 free base ( PF05089771 free base )
产品货号. M10943 CAS No. 1235403-62-9
PF-05089771 free base 是一种有效的亚型选择性 Nav1.7 抑制剂,IC50 为 11 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ¥1454 | 有现货 |
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| 10MG | ¥1834 | 有现货 |
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| 25MG | ¥3041 | 有现货 |
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| 50MG | ¥4343 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
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| 1G | 获取报价 | 有现货 |
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| 1 mL x 10 mM in DMSO | ¥1606 | 有现货 |
|
生物学信息
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产品名称PF-05089771 free base
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述PF-05089771 free base 是一种有效的亚型选择性 Nav1.7 抑制剂,IC50 为 11 nM。
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产品描述PF-05089771 free base is a potent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, shows no activity against Nav 1.5 and >10-fold selectivity over other Nav isoforms; specifically interacts with the voltage-sensor domain (VSD4); blocks the majority of TTX-S current (75%) at 30 nM in human DRG neurons (IC50=8.4 nM); exhibits action potentials in spinal slice electrophysiology recordings, mouse and human DRG neurons, demonstrates in vivo efficacy mouse capsaicin-induced neurogenic flare model.
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体外实验PF-05089771 is determined to be more than 1000-fold selective over tetrodotoxin-resistant (TTX-R) Nav1.5 and Nav1.8 channels (IC50s >10 μM) and exhibited a range of selectivity over TTX-sensitive (TTX-S) channels (10-fold for Nav1.2 to 900-fold for Nav1.3 and Nav1.4).PF-05089771 (30 nM) blocks the majority of TTX-S current (75.5 ± 10.5%, n = 5, Fig 5D) whilst 100 nM resulted in complete block.
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体内实验——
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同义词PF05089771 free base
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通路Membrane Transporter/Ion Channel
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靶点Sodium Channel
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受体Sodium Channel
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研究领域Neurological Disease
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适应症Pain
化学信息
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CAS Number1235403-62-9
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分子量500.354
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分子式C18H12Cl2FN5O3S2
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纯度>98% (HPLC)
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溶解度DMSO: ≥ 34 mg/mL
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SMILESC1=CC(=C(C=C1Cl)C2=C(NN=C2)N)OC3=CC(=C(C=C3Cl)S(=O)(=O)NC4=CSC=N4)F
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化学全称Benzenesulfonamide, 4-[2-(3-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-4-thiazolyl-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
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Benzamil (hydrochlor...
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Silperisone HCl
Silperisone HCl (RGH-5002) blocks sodium and calcium channels in cells, decreases excitability and contractility of muscle cells, reduces peripheral tone, and acts as a muscle relaxant and peripheral vasodilator. Silperisone HCl is used to treat recurrent painful myoclonus due to spinal cord injury, abnormal hypertonia due to cerebrovascular disease, dystonia symptoms, cone tension syndrome, multiple sclerosis myospasm and myelitis. silperisone is a sodium channel protein type 2 alpha channel blocker. silperisone is an organosilicon similar to tolperisone, an organosilicon compound with centrally acting muscle relaxant properties.
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5-Tridecanol
5-Tridecanol blocks ion flux in sodium channels.
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