GNE-131

目录号: PL11375 纯度: ≥98%
GNE-131 是人类钠离子通道 NaV1.7 (hNaV1.7) 有效的、选择性抑制剂,其 IC50 值为 3 nM。
CAS No. :1629063-81-5
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中文名称
GNE-131
中文别名
化合物GNE-131
英文名称
GNE-131
英文别名
GNE-131;gne-131;GNE131;GNE 131;CS-2887;Cyclopropanesulfonamide, N-[6-cyclopropyl-7-(tricyclo[3.3.1.13,7]dec-1-ylmethoxy)-1,2,4-triazolo[4,3-a]pyridin-3-yl]-;N-[6-Cyclopropyl-7-(tricyclo[3.3.1.13,7]dec-1-ylmethoxy)-1,2,4-triazolo[4,3-a]pyridin-3-yl]cyclopropanesulfonamide
Cas No.
1629063-81-5
分子式
C23H30N4O3S
分子量
442.57
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
GNE-131 是人类钠离子通道 NaV1.7 (hNaV1.7) 有效的、选择性抑制剂,其 IC50 值为 3 nM。
产品详情
GNE-131 是人类钠离子通道 NaV1.7 (hNaV1.7) 有效的、选择性抑制剂,其 IC50 值为 3 nM。
生物活性
GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC 50 of 3 nM.
性状
Solid
IC50 & Target[1][2]
Nav1.7 3 nM (IC50)
体外研究(In Vitro)
GNE-131 (Compound 13) shows moderate clearance in human liver microsomes and excellent functional activity against human NaV1.7 with an IC50 of 0.003±0.001 μM. GNE-131 shows excellent potency, good in vitro metabolic stability. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GNE-131 shows low in vivo clearance in mouse, rat, and dog. GNE-131 also displays excellent efficacy in a transgenic mouse model of induced pain. has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Focken T, et al. Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain. J Med Chem. 2018 Jun 14
溶解度数据
In Vitro: DMSO : 125 mg/mL (282.44 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Focken T, et al. Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain. J Med Chem. 2018 Jun 14

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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