Ampreloxetine

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) 是一种有效的单胺再摄取抑制剂，对人 NET、SERT 和 DAT 的 pIC50 分别为 8.0、8.6 和 6.8。

Ampreloxetine (TD-9855) is a potent monoamine reuptake inhibitor with pIC50 of 8.0, 8.6 and 6.8 for human NET, SERT, and DAT, respectively; displays an inhibitory selectivity of 4- to 10-fold for NE at human and rat transporter; engaged norepinephrine transporters (NET) and serotonin transporters (SERT) in rat spinal cord, with a plasma EC50 of 11.7 ng/mL and 50.8 ng/mL, respectively; TD-9855 is an investigational dual norepinephrine (NE) and serotonin (5-HT) reuptake inhibitor with selectivity for NE over 5-HT (NSRI).Other Indication Phase 2 Clinical.

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Animal Model:Male Sprague Dawley rats Dosage:0.3, 1, 5, 10, 30, 60 mg/kg Administration:P.o.; single dose Result:Showed good PK and PD parameter with Emax of 79%, 92% for SERT and NET, respectively; EC50 values of 50.8, 11.7 ng/mL for SERT, NET, respectively.

TD-9855 | TD9855

Membrane Transporter/Ion Channel

Monoamine Transporter

Monoamine Transporter

Other Indications

Other Disease

1227056-84-9

321.343

C18H18F3NO

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (311.20 mM)

FC1=C(OCC2=CC=CC=C2C3CCNCC3)C(F)=CC(F)=C1.[H]Cl

4-{2-[(2,4,6-trifluorophenoxy)methyl]phenyl}piperidine

(-20℃)

With Ice Pack

≥ 2 years