产品
编 号：F743313
分子式：C18H19ClF3NO
分子量：357.8
分子式：C18H19ClF3NO
分子量：357.8
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 1227056-87-2
产品详情
生物活性：
Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma.
体内研究：
Ampreloxetine hydrochloride (0.3- 60mg /kg；口服；单剂量) 在大鼠模型中，其血浆浓度和剂量水平无关。Animal Model:Rat
Dosage:0.3, 1, 5, 10, 30, and 60mg/kg
Administration:PO; euthanized by decapitation at 0.5, 2, 4, 6, and 8 hr for 5mg/ kg dose level; 2 hr for 0.3, 1, 10, 30, and 60mg/kg dose levels
Result:In the effect compartment PK/PD analysis for NET and SERT occupancy, the estimated EC50 for occupancy was 11.7ng/mL for NET and 50.8ng/mL for SERT in rat spinal cords, and the projected human plasma EC50 values were 5.5ng/mL for NET and 23.9ng/mL for SERT.
Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma.
体内研究：
Ampreloxetine hydrochloride (0.3- 60mg /kg；口服；单剂量) 在大鼠模型中，其血浆浓度和剂量水平无关。Animal Model:Rat
Dosage:0.3, 1, 5, 10, 30, and 60mg/kg
Administration:PO; euthanized by decapitation at 0.5, 2, 4, 6, and 8 hr for 5mg/ kg dose level; 2 hr for 0.3, 1, 10, 30, and 60mg/kg dose levels
Result:In the effect compartment PK/PD analysis for NET and SERT occupancy, the estimated EC50 for occupancy was 11.7ng/mL for NET and 50.8ng/mL for SERT in rat spinal cords, and the projected human plasma EC50 values were 5.5ng/mL for NET and 23.9ng/mL for SERT.
产品资料
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