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Description: Potent and selective negative allosteric modulator of mGlu1 receptors
Chemical Name: 4-Fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide
Purity: ≥98% (HPLC)
Biological Activity for FITM
FITM is a potent and selective negative allosteric modulator of mGlu1 receptors (IC50 = 5.1 nM). Displays >1300-fold selectivity for mGlu1 over other metabotropic glutamate receptors (IC50 values are 7 μM and >10 μM for mGlu5 and mGlu2 or mGlu8, respectively). Antagonizes methamphetamine-induced locomotion in mice.
Compound Libraries for FITM
FITM is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for FITM
| M. Wt | 371.43 |
| Formula | C18H18FN5OS |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 932737-65-0 |
| PubChem ID | 16660135 |
| InChI Key | WIVGIKIKQHUFOD-UHFFFAOYSA-N |
| Smiles | CC(C)NC1=CC(=NC=N1)C1=CSC(=N1)N(C)C(=O)C1=CC=C(F)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for FITM
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.14 | 100 | |
| ethanol | 7.43 | 20 |
Preparing Stock Solutions for FITM
The following data is based on the product molecular weight 371.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.69 mL | 13.46 mL | 26.92 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.38 mL |
| 10 mM | 0.27 mL | 1.35 mL | 2.69 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
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Product Datasheets for FITM
References for FITM
References are publications that support the biological activity of the product.
Satoh et al (2009) Discovery and in vitro and in vivo profiles of 4-fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as novel class of an orally active metabotropic glutamate receptor 1 (mGluR1) antagonist. Bioorg.Med.Chem.Lett. 19 5464 PMID: 19674894
Wu et al (2014) Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Science. 344 58 PMID: 24603153
If you know of a relevant reference for FITM, please let us know.
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Keywords: FITM, FITM supplier, potent, selective, negative, allosteric, modulator, antagonist, mGlu1, group, I, metabotropic, glutamate, receptor, Glutamate, (Metabotropic), Group, Receptors, 6859, Tocris Bioscience
Citations for FITM
Citations are publications that use Tocris products.
Currently there are no citations for FITM. Do you know of a great paper that uses FITM from Tocris? Please let us know.
Reviews for FITM
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Metabotropic Glutamate Receptors Scientific Review
Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.
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