| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| N655081-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $341.90 |
| Specifications & Purity | 10mM in DMSO |
|---|---|
| Biochemical and Physiological Mechanisms | Nav1.1 activator 1 (compound 4), a highly potent Na v 1.1 activator with BBB penetration , increases decay time constant (tau) of Na v 1.1 currents at 0.03 μM along with significant selectivity against Na v 1.2, Na v 1.5, and Na v 1.6. |
| Storage Temp | Store at -80°C |
| Shipped In | Ice chest + Ice pads |
| Product Description | Nav1.1 activator 1 (compound 4), a highly potent Na v 1.1 activator with BBB penetration , increases decay time constant (tau) of Na v 1.1 currents at 0.03 μM along with significant selectivity against Na v 1.2, Na v 1.5, and Na v 1.6 In Vivo Nav1.1 activator 1 (compound 4) is a valuable Na v 1.1 activator for further evaluation of pathophysiological functions of the Nav1.1 channel and has potential for therapeutic treatments of CNS diseases such as Dravet syndrome . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice . Dosage: 30 mg/kg ( Pharmacokinetic Analysis ). Administration: IP once (Exposure was measured at 1 h after administration). Result: Intraperitoneal administration (30 mg/kg) of compound resulted in sufficient brain exposure (193 ng/g 1 h after administration), which corresponded to 13 nM of free brain concentration comparable to the in vitro potency of the compound. Had a potential use as an in vivo tool to investigate whether this type of Na v 1.1 activator can restore Na v 1.1 functions and modify the disease state in animal models. Could penetrate the blood-brain barrier (BBB) in humans. IC50& Target:Na v 1.1 |
| Canonical SMILES | O=C(C1=C(C2=CC(F)=CC=C2F)C=CN=C1N3C[C@@H](F)CC3)NC4=CC=C(C(C)C)N=C4 |
|---|---|
| Molecular Weight | 440.46 |
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