| Identification | Back Directory | [Name]
FITM | [CAS]
932737-65-0 | [Synonyms]
FITM
4-Fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide
Benzamide, 4-fluoro-N-methyl-N-[4-[6-[(1-methylethyl)amino]-4-pyrimidinyl]-2-thiazolyl]- | [Molecular Formula]
C18H18FN5OS | [MOL File]
932737-65-0.mol | [Molecular Weight]
371.43 |
| Chemical Properties | Back Directory | [Boiling point ]
573.9±60.0 °C(Predicted) | [density ]
1.334±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 100mM; Ethanol: 20mM | [form ]
A crystalline solid | [pka]
3.03±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
4-Fluoro-N-methyl-N-[4-[6-[(1-methylethyl)amino]-4-pyrimidinyl]-2-thiazolyl]benzamide is a potent mGluR1 antagonist. It also demonstrats a relatively potent antipyschotic-like effect in several animal models, suitable for the development of a PET tracer. | [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]. | [IC 50]
mGlu1: 2.5 nM (Ki) | [storage]
Store at -20°C |
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