1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. FPTQ

FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo.

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

FPTQ Chemical Structure

FPTQ Chemical Structure

CAS No. : 864863-72-9

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 253 In-stock
Solution
10 mM * 1 mL in DMSO USD 253 In-stock
Solid
5 mg USD 230 In-stock
10 mg USD 330 In-stock
25 mg USD 660 In-stock
50 mg USD 890 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively[1]. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo[2].

IC50 & Target[1]

Human mGluR1

6 nM (IC50)

Mouse mGluR1

1.4 nM (IC50)

In Vitro

FPTQ (0.5-10 μM) does not shows any cytotoxicity was not observed at 0.5, 1, 5, and 10 μM in RAW264.7 macrophage cells[2].
FPTQ (1-20 μM; 24 hours) reduces LPS-induced NO production at > 1 μM FPTQ, and at 10 μM, FPTQ treatment causes a 31% anti-oxidant effect in RAW264.7 macrophage cells[2].
FPTQ (1-20 μM; 24 hours) dramaticly decreases LPS-induced expression levels of IL-1β and Il-6. At a concentration of 10 μM, FPTQ causes a 27% and 44% reduction in the mRNA expression of IL-1β and Il-6, respectively in RAW264.7 macrophage cells[2].

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

RT-PCR[1]

Cell Line: RAW264.7 macrophage cells
Concentration: 1, 10, or 20 μM
Incubation Time: 24 hours
Result: Decreased IL-1β and IL-6 mRNA expression
In Vivo

FPTQ (5-20 μM) decreases the number of neutrophils migrating to the amputation site in zebrafish larvae by tail amputation. In the tailfin wound method, the number of neutrophils collecting at the wound site also decreases in a dose-dependent manner in zebrafish[2].
In a LPS-induced inflammation zebrafish model, LPS solution is injected into the yolks of Tg(mpx:EGFP)i114 zebrafish larvae and exposed the zebrafish larvae immediately to FPTQ treatment.
FPTQ (20 μM; 4 hours) significantly decreases the fluorescent neutrophils after yolk injection and has an anti-inflammatory effect during the early phase of inflammation[2].

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

Molecular Weight

305.31

Formula

C17H12FN5

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC(N=CC=C1)=C1N2N=NC(C3=CC4=C(C=C3)N=CC=C4)=C2C

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 (109.17 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 3.2754 mL 16.3768 mL 32.7536 mL
5 mM 0.6551 mL 3.2754 mL 6.5507 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: ≥ 2.5 mg/mL (8.19 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 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.
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 3.2754 mL 16.3768 mL 32.7536 mL 81.8840 mL
5 mM 0.6551 mL 3.2754 mL 6.5507 mL 16.3768 mL
10 mM 0.3275 mL 1.6377 mL 3.2754 mL 8.1884 mL
15 mM 0.2184 mL 1.0918 mL 2.1836 mL 5.4589 mL
20 mM 0.1638 mL 0.8188 mL 1.6377 mL 4.0942 mL
25 mM 0.1310 mL 0.6551 mL 1.3101 mL 3.2754 mL
30 mM 0.1092 mL 0.5459 mL 1.0918 mL 2.7295 mL
40 mM 0.0819 mL 0.4094 mL 0.8188 mL 2.0471 mL
50 mM 0.0655 mL 0.3275 mL 0.6551 mL 1.6377 mL
60 mM 0.0546 mL 0.2729 mL 0.5459 mL 1.3647 mL
80 mM 0.0409 mL 0.2047 mL 0.4094 mL 1.0235 mL
100 mM 0.0328 mL 0.1638 mL 0.3275 mL 0.8188 mL
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FPTQ 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.

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