| CAS NO: | 1629063-81-5 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 1629063-81-5 |
| Canonical SMILES | O=S(NC1=NN=C2N1C=C(C3CC3)C(OCC45C[C@@H](C6)C[C@@H](C[C@@H]6C5)C4)=C2)(C7CC7)=O |
| 分子式 | C23H30N4O3S |
| 分子量 | 442.57 |
| 溶解度 | DMSO : 125 mg/mL (282.44 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM. 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[1]. 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[1]. [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;61(11):4810-4831. |
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