SSR504734 HCl

Research use only, not for human use.

SSR504734 is an orally active, selective, and reversible inhibitor of human, rat, and mouse GlyT1 (IC50 = 18, 15, and 38 nM, respectively). SSR504734 exhibits activity in schizophrenia, anxiety, and depression models .

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.

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Others

Other Targets

Others

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615571-23-8

433.3

C20H21Cl2F3N2O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (230.79 mM; Ultrasonic )

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

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(-20℃)

With Ice Pack

≥ 2 years