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

FITM 

Cat. No.: HY-101845 Purity: 98.19%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 74 In-stock
Estimated Time of Arrival: December 31
2 mg USD 50 In-stock
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5 mg USD 90 In-stock
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10 mg USD 150 In-stock
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25 mg USD 300 In-stock
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50 mg USD 500 In-stock
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100 mg USD 850 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

Ki: 2.5 nM (mGlu1)[1]

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].

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].

Molecular Weight

371.43

Formula

C₁₈H₁₈FN₅OS

CAS No.

932737-65-0

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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (403.84 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2692 mL 1.3461 mL 2.6923 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

FITMmGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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FITM
Cat. No.:
HY-101845
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