GNE-616
- CAS No.
- 2349371-81-7
- Chemical Name:
- GNE-616
- Synonyms
- GNE-616;GNE616,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)-
- CBNumber:
- CB95821427
- Molecular Formula:
- C24H23F4N5O3S
- Molecular Weight:
- 537.53
- MDL Number:
- MFCD32197241
- MOL File:
- 2349371-81-7.mol
GNE-616 Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
GNE-616 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9730 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24131 | 58 |
Supplier | Advantage |
---|---|
TargetMol Chemicals Inc. | 58 |
Fan De(Beijing) Biotechnology Co., Ltd. | 58 |
TargetMol Chemicals Inc. | 58 |