产品
编 号：F618702
分子式：C24H23F3N4O
分子量：440.46
分子式：C24H23F3N4O
分子量：440.46
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
询价
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10mg
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结构图
CAS No: 2332897-85-3
产品详情
生物活性：
Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.
体内研究：
Nav1.1 activator 1 (compound 4) 是一种有价值的 Nav1.1 激活剂，可用于进一步评估 Nav1.1 通道的病理生理功能，并具有处理 Dravet 综合征等中枢神经系统疾病的潜力。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 Nav1.1 activator can restore Nav1.1 functions and modify the disease state in animal models.Could penetrate the blood-brain barrier (BBB) in humans.
Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.
体内研究：
Nav1.1 activator 1 (compound 4) 是一种有价值的 Nav1.1 激活剂，可用于进一步评估 Nav1.1 通道的病理生理功能，并具有处理 Dravet 综合征等中枢神经系统疾病的潜力。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 Nav1.1 activator can restore Nav1.1 functions and modify the disease state in animal models.Could penetrate the blood-brain barrier (BBB) in humans.
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