SSR504734 HCl

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

SSR504734 是一种具有口服活性、选择性和可逆性的 GlyT1 抑制剂 (hGlyT1，rGlyT1，mGlyT1 IC50 分别为 18、15 和 38 nM)。SSR504734 表现出抗精神分裂、抗焦虑和抗抑郁的活性。

SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38?nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities.

SSR504734 (15 nM-86 μM; 10 min) inhibits glycine uptake in human SK-N-MC and rat C6 cells.Cell Viability Assay Cell Line:Human neuroblastoma (SK-N-MC) and rat astrocytoma (C6) cells Concentration:15 nM-86 μM Incubation Time:10 min Result:Showed IC50 values of 18 and 15 nM for human SK-N-MC and rat C6 cells, respectively.

SSR504734 (i.p. and p.o.; 1-100 mg/kg; once) treatment shows good oral bioavailability.SSR504734 (i.p.; 30 mg/kg; once) induces a rapid and significant decrease of specific glycine uptake.SSR504734 (i.p.; 10 mg/kg; once) increases extracellular levels of Glycine in the prefrontal cortex (PFC) of freely moving rats.Animal Model:Male Sprague-Dawley rats Dosage:1-100 mg/kg Administration:Intraperitoneal injection and oral gavage.; 1-100 mg/kg; once Result:Showed ID50 values of 5.0 and 4.6?mg/kg for i.p. and p.o. treatments, respectively.Animal Model:Male Sprague-Dawley rats Dosage:30 mg/kg Administration:Intraperitoneal injection; 30 mg/kg; once Result:Maintained at about 80% inhibition from 1 to 7?h after administration.Animal Model:Male Sprague-Dawley ratsDosage:10 mg/kg Administration:Intraperitoneal injection; 10 mg/kg; once Result:Produced a rapid and sustained increase in PFC extracellular levels of glycine.

——

Others

Other Targets

Others

——

——

615571-23-8

433.3

C20H21Cl2F3N2O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (230.79 mM; 超声助溶 )

Cl.[H][C@]1(CCCCN1)[C@@H](NC(=O)c1cccc(c1Cl)C(F)(F)F)c1ccccc1

——

(-20℃)

With Ice Pack

≥ 2 years