| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:GNE-616
CAS:2349371-81-7
Package:100mg/RMB 39500;50mg/RMB 30300;25mg/RMB 22700
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| | GNE-616 Basic information |
| Product Name: | GNE-616 | | Synonyms: | GNE-616;2H-1-Benzopyran-7-sulfonamide, 6-fluoro-3,4-dihydro-4-[(2R,4S)-2-(2-pyridinyl)-4-(trifluoromethyl)-1-piperidinyl]-N-4-pyrimidinyl-, (4S)-;GNE616,GNE 616 | | CAS: | 2349371-81-7 | | MF: | C24H23F4N5O3S | | MW: | 537.53 | | EINECS: | | | Product Categories: | | | Mol File: | 2349371-81-7.mol |  |
| | GNE-616 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Soluble in DMSO |
| | GNE-616 Usage And Synthesis |
| Description | GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively[1].
Ki: 0.79 nM (hNav1.7)[1]Kd: 0.38 nM (hNav1.7), 12 nM (hNav1.2), 29 nM (hNav1.6)[1] Site-directed mutagenesis is critical for the isoform selectivity profile of GNE-616 (hNav1.7, Kd: Y1537s/W1538=170±67 nM, V1541=3.9±1.1 nM, Y1537s/W1538/V1541=790±350 nM)[1]. GNE-616 shows robust activity in a Nav1.7-dependent inherited erythromelalgia (IEM) PK/PD model with an EC50 of 740 nM and EC50,u of 9.6 nM[1]. | | References | [1]. McKerrall SJ, et al. Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain. J Med Chem. 2019 Apr 25;62(8):4091-4109. |
| | GNE-616 Preparation Products And Raw materials |
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