1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GlyT
  3. SSR504734

SSR504734 

Cat. No.: HY-10715
Handling Instructions

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.

For research use only. We do not sell to patients.

SSR504734 Chemical Structure

SSR504734 Chemical Structure

CAS No. : 615571-23-8

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Description

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[1].

IC50 & Target

hGlyT1

18 nM (IC50)

rGlyT1

15 nM (IC50)

In Vitro

SSR504734 (15 nM-86 μM; 10 min) inhibits glycine uptake in human SK-N-MC and rat C6 cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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.
In Vivo

SSR504734 (i.p. and p.o.; 1-100 mg/kg; once) treatment shows good oral bioavailability[1].
SSR504734 (i.p.; 30 mg/kg; once) induces a rapid and significant decrease of specific glycine uptake[1].
SSR504734 (i.p.; 10 mg/kg; once) increases extracellular levels of Glycine in the prefrontal cortex (PFC) of freely moving rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats[1]
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[1]
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 rats[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 10 mg/kg; once
Result: Produced a rapid and sustained increase in PFC extracellular levels of glycine.
Molecular Weight

433.29

Formula

C20H21Cl2F3N2O

CAS No.
SMILES

O=C(C1=C(C(C(F)(F)F)=CC=C1)Cl)N[[email protected]]([[email protected]]2([H])CCCCN2)C3=CC=CC=C3.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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