2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. FITM

FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.

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

FITM Chemical Structure

FITM Chemical Structure

CAS No. : 932737-65-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 120 In-stock
25 mg USD 240 In-stock
50 mg USD 360 In-stock
100 mg USD 530 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

FITM Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE FITM

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

FITM is a negative allosteric modulator of mGlu1 receptor with a Ki of 2.5 nM.

IC50 & Target[1]

mGlu1

2.5 nM (Ki)

In Vitro

FITM fits tightly into the long and narrow pocket. Most of the ligand-receptor interactions are hydrophobic with the exception of the contacts of the pyrimidine-amine group with the T815 7.38 side chain. The mGlu1 binding pocket for FITM largely corresponds to mutagenic data for the common allosteric site in mGlus and likely extends to other class C GPCRs. FITM which shows high affinity and selectivity for mGlu1 over mGlu5[1]. FITM has the high hydrogen bonds occupancy with Thr815 and Tyr805 in dimer A and B of mGlu1 during molecular dynamics simulations. The nitrogen and hydrogen atoms of FITM form the dynamical hydrogen bonds with the hydrogen atom of Tyr805 and oxygen atom of Thr815, respectively. It indicates that there is a strong attraction interaction between FITM and allosteric sites[2].

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

FITM Related Antibodies
In Vivo

The pretreatment of rats with unlabeled FITM (1 mg/kg) occupies an mGluR1 binding site of 18F-FITM by more than 99% and does not affect the input function. The Kd (nM) and Bmax (pmol/mL) obtained by the Scatchard analyses with the multidose ligand assays are 2.1 and 36.3, respectively, for the thalamus; 2.1 and 27.5, respectively, for the hippocampus; 1.5 and 22.2, respectively, for the striatum; and 1.5 and 20.5, respectively, for the cingulate cortex with a high confidence[3]. 18F-FITM shows excellent pharmacokinetics, namely the dense and specific accumulation in mGlu1-positive melanomas versus mGlu1-negative hepatoma and normal tissues. Furthermore, the accumulation levels of radioactivity corresponded to the extent of tumor and to levels of mGlu1 protein expression in melanomas and melanoma metastasis[4].

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

371.43

Formula

C18H18FN5OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(C)C1=NC(C2=NC=NC(NC(C)C)=C2)=CS1)C3=CC=C(F)C=C3
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 : 100 mg/mL (269.23 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 2.6923 mL 13.4615 mL 26.9230 mL
5 mM 0.5385 mL 2.6923 mL 5.3846 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 (6.73 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 2.6923 mL 13.4615 mL 26.9230 mL 67.3074 mL
5 mM 0.5385 mL 2.6923 mL 5.3846 mL 13.4615 mL
10 mM 0.2692 mL 1.3461 mL 2.6923 mL 6.7307 mL
15 mM 0.1795 mL 0.8974 mL 1.7949 mL 4.4872 mL
20 mM 0.1346 mL 0.6731 mL 1.3461 mL 3.3654 mL
25 mM 0.1077 mL 0.5385 mL 1.0769 mL 2.6923 mL
30 mM 0.0897 mL 0.4487 mL 0.8974 mL 2.2436 mL
40 mM 0.0673 mL 0.3365 mL 0.6731 mL 1.6827 mL
50 mM 0.0538 mL 0.2692 mL 0.5385 mL 1.3461 mL
60 mM 0.0449 mL 0.2244 mL 0.4487 mL 1.1218 mL
80 mM 0.0337 mL 0.1683 mL 0.3365 mL 0.8413 mL
100 mM 0.0269 mL 0.1346 mL 0.2692 mL 0.6731 mL
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FITM 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:

FITM932737-65-0mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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