PF-05198007

目录号: PL11344 纯度: ≥99%
PF-05198007 是有效的、具有口服活性的、选择性的 Nav1.7 丙烯酰胺抑制剂。PF-05198007 和PF-05089771 (HY-12883) 具有相似的药效学特征。
CAS No. :1235406-19-5
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中文名称
PF-05198007
英文名称
PF-05198007
英文别名
4-(2-(3-Amino-1H-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide;BDBM50257214;4-[2-(3-amino-1h-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy]-5-chloro-2-fluoro-n-1,3-thiazol-4-ylbenzenesulfonamide;4-[2-(5-amino-1H-pyrazol-4-yl)-4-(trifluoromethyl)phenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide;PF-05198007
Cas No.
1235406-19-5
分子式
C19H12ClF4N5O3S2
分子量
533.91
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
PF-05198007 是有效的、具有口服活性的、选择性的 Nav1.7 丙烯酰胺抑制剂。PF-05198007 和PF-05089771 (HY-12883) 具有相似的药效学特征。
产品详情
PF-05198007 是有效的、具有口服活性的、选择性的 Nav1.7 丙烯酰胺抑制剂。PF-05198007 和PF-05089771 (HY-12883) 具有相似的药效学特征。
生物活性
PF-05198007 is a potent, orally active and selective arylsulfonamide Na v 1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771.
性状
Solid
IC50 & Target[1][2]
Nav1.7
体外研究(In Vitro)
PF-05198007 (30 nM) blocks on average 83.0 ± 2.7% of the total TTX-S current indicating that the major TTX-S conductance is carried through Nav1.7 channels in small-diameter mouse DRG neurons (n = 35). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PF-05198007 (1 or 10 mg/kg, orally) reduces the capsaicin flare response in WT, but not Na v 1.7Na v mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult Mal
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405.
[2]. Kushnarev M, et al. Neuropathic pain: preclinical and early clinical progress with voltage-gated sodium channel blockers. Expert Opin Investig Drugs. 2020 Mar;29(3):259-271.
溶解度数据
In Vitro: DMSO : 150 mg/mL (280.95 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Alexandrou AJ, et al. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release. PLoS One. 2016 Apr 6;11(4):e0152405.
[2]. Kushnarev M, et al. Neuropathic pain: preclinical and early clinical progress with voltage-gated sodium channel blockers. Expert Opin Investig Drugs. 2020 Mar;29(3):259-271.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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