GNE-131 - Sodium Channel 抑制劑 - 生命科學試劑 - 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作靶點: Sodium Channel作通路: Membrane Transporter/Ion Channel儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 125 mg/mL (282.44 m

2、M; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結果的可靠性，體內實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備

3、液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.70 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.70 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL

4、 (4.70 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 GNE-131類鈉離通道 NaV1.7 (hNaV1.7) 有效的、選擇性抑制劑，其 IC50 值為 3 nM。IC50 & Target IC50: 3 nM (hNaV1.7) 1.體外研究 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.體內研究 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-