Ampreloxetine hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ampreloxetine (TD-9855) hydrochloride 是一种具有口服活性和 CNS 渗透性的去甲肾上腺素转运体 (NET) 和羟色胺 5-HT 摄取转运体 (SERT) 抑制剂，但不是多巴胺转运蛋白 (DAT)。Ampreloxetine hydrochloride结合去 NET 和 SERT，在血浆中的 EC50 值分别为 11.7 ng/mL 和 50.8 ng/mL。

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.

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Animal Model:RatDosage: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.

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Others

Other Targets

Others

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1227056-87-2

357.8

C18H19ClF3NO

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (279.49 mM; 超声助溶 )

Cl.FC=1C=C(F)C(OCC=2C=CC=CC2C3CCNCC3)=C(F)C1

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(-20℃)

With Ice Pack

≥ 2 years