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

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.

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SSR504734 Chemical Structure

SSR504734 Chemical Structure

CAS No. : 615571-23-8

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Based on 1 publication(s) in Google Scholar

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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].

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

SSR504734 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (230.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3079 mL 11.5396 mL 23.0792 mL
5 mM 0.4616 mL 2.3079 mL 4.6158 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.77 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3079 mL 11.5396 mL 23.0792 mL 57.6981 mL
5 mM 0.4616 mL 2.3079 mL 4.6158 mL 11.5396 mL
10 mM 0.2308 mL 1.1540 mL 2.3079 mL 5.7698 mL
15 mM 0.1539 mL 0.7693 mL 1.5386 mL 3.8465 mL
20 mM 0.1154 mL 0.5770 mL 1.1540 mL 2.8849 mL
25 mM 0.0923 mL 0.4616 mL 0.9232 mL 2.3079 mL
30 mM 0.0769 mL 0.3847 mL 0.7693 mL 1.9233 mL
40 mM 0.0577 mL 0.2885 mL 0.5770 mL 1.4425 mL
50 mM 0.0462 mL 0.2308 mL 0.4616 mL 1.1540 mL
60 mM 0.0385 mL 0.1923 mL 0.3847 mL 0.9616 mL
80 mM 0.0288 mL 0.1442 mL 0.2885 mL 0.7212 mL
100 mM 0.0231 mL 0.1154 mL 0.2308 mL 0.5770 mL
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SSR504734 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SSR504734615571-23-8SSR 504734SSR-504734GlyTGlycine transportersoral activityanti-schizophrenia activityanti-anxiety activityanti-depression activitySK-N-MCC6Inhibitorinhibitorinhibit

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