2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GlyT
  4. PF-03463275

PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.

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

PF-03463275 Chemical Structure

PF-03463275 Chemical Structure

CAS No. : 1173239-39-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 240 In-stock
50 mg USD 600 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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GlyT1 GlyT2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research[1][2].

In Vivo

PF-03463275 (1-10 mg/kg; s.c.) attenuates oscillatory potentials (OPs)[2].

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

Animal Model: Male Sprague-Dawley rats[2]
Dosage: 1, 3 and 10 mg/kg
Administration: S.c.
Result: A dose-dependent reduction in the amplitude of oscillatory potentials (OPs) elicited from the dark-adapted rats.
Clinical Trial
Molecular Weight

376.86

Formula

C19H22ClFN4O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C(N=C1)=CN1C)N(CC(C=C2)=CC(Cl)=C2F)C[C@@H]3[C@](C4)([H])[C@@]3([H])CN4C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (88.44 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 2.6535 mL 13.2675 mL 26.5351 mL
5 mM 0.5307 mL 2.6535 mL 5.3070 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 0.83 mg/mL (2.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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: ≥ 0.83 mg/mL (2.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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).
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6535 mL 13.2675 mL 26.5351 mL 66.3376 mL
5 mM 0.5307 mL 2.6535 mL 5.3070 mL 13.2675 mL
10 mM 0.2654 mL 1.3268 mL 2.6535 mL 6.6338 mL
15 mM 0.1769 mL 0.8845 mL 1.7690 mL 4.4225 mL
20 mM 0.1327 mL 0.6634 mL 1.3268 mL 3.3169 mL
25 mM 0.1061 mL 0.5307 mL 1.0614 mL 2.6535 mL
30 mM 0.0885 mL 0.4423 mL 0.8845 mL 2.2113 mL
40 mM 0.0663 mL 0.3317 mL 0.6634 mL 1.6584 mL
50 mM 0.0531 mL 0.2654 mL 0.5307 mL 1.3268 mL
60 mM 0.0442 mL 0.2211 mL 0.4423 mL 1.1056 mL
80 mM 0.0332 mL 0.1658 mL 0.3317 mL 0.8292 mL
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PF-03463275 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:

PF-034632751173239-39-8PF03463275PF 03463275GlyTGlycine transporterscognitivesymptomsschizophreniaoralCNSSprague-DawleyratInhibitorinhibitorinhibit

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