FITM
FITM Basic information
- Product Name:
- FITM
- 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]-
- 4-fluoro-N-methyl-N-[4-[6-(propan-2-ylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]benzamide
- FITM,mGluR,Metabotropic glutamate receptors,inhibit,Inhibitor
- 4-Fluoro-N-(4-(6-(isopropylamino)pyrimidin-4-yl)thiazol-2-yl)-N-methylbenzamide
- FITM, 10 mM in DMSO
- CAS:
- 932737-65-0
- MF:
- C18H18FN5OS
- MW:
- 371.43
- Mol File:
- 932737-65-0.mol
FITM Chemical Properties
- 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
FITM Usage And Synthesis
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
FITMSupplier
- Tel
- sales@boylechem.com
- Tel
- 025-66028182 18626450290
- yftan@aikonchem.com
- Tel
- 021-52996696，15000506266 15000506266
- Tel
- 022-60688926
- Tel
- 515-88280676 18921872653
- sales@ximanbio.com