GNE-131 - Sodium Channel 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGNE-131Cat. No.: HY-112279CAS No.: 1629063-81-5分式: CHNOS分量: 442.57作靶点: Sodium Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (282.44 m

2、M; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2595 mL 11.2976 mL 22.5953 mL5 mM 0.4519 mL 2.2595 mL 4.5191 mL10 mM 0.2260 mL 1.1298 mL 2.2595 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备

3、液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.70 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.70 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL

4、 (4.70 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 GNE-131类钠离通道 NaV1.7 (hNaV1.7) 有效的、选择性抑制剂，其 IC50 值为 3 nM。IC50 & Target IC50: 3 nM (hNaV1.7) 1.体外研究 GNE-131 (Compound 13) shows moderate clearance in human liver microsomes and excellent functionalactivit

5、y against human NaV1.7 with an IC50 of 0.0030.001 M. GNE-131 shows excellent potency, good invitro metabolic stability 1.体内研究 GNE-131 shows low in vivo clearance in mouse, rat, and dog. GNE-131 also displays excellent efficacy in atransgenic mouse model of induced pain 1.REFERENCES1. Focken T, et al

6、. Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-(1,2,4Triazolo4,3- apyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain. J Med Chem. 2018 Jun 14;61(11):4810-4831.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-