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GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM. GNE-131 shows excellent potency, good in vitro metabolic stability.
In vivo, 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.
| Molecular Weight | 442.57 |
| Formula | C23H30N4O3S |
| CAS Number | 1629063-81-5 |
| Solubility (25°C) | DMSO: ≥ 90 mg/mL (Need ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Sodium Channel Products |
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5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively. |
| HwTx-IV
Huwentoxin-IV (HwTx-IV) is a 35-residue neurotoxin peptide with potential application as a novel analgesic. Huwentoxin-IV, a component of tarantula venom, potently blocks sodium channels and is an attractive scaffold for engineering a Nav1.7-selective molecule. |
| ST-2560
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