| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 4-fluoro-N-methyl-N-[4-[6-(propan-2-ylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]benzamide.
- CAS number: 932737-65-0
- Molecular formula: C18H18FN5OS.
- Purity: >99%
- Concentration: 1-100 nM.
- Form: Lyophilized powder.
- Solubility: Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
- Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. For long-term storage of diluted solutions, we recommend adding 0.1% BSA. Repeat freeze-thawing may result in loss of activity.
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: mGluR1
- Source: Synthetic
- Activity: FITM is a potent, noncompetitive antagonist of mGluR1 receptors (IC50 = 5.1 nM), selective over mGluR5 (IC50 = 7000 nM), mGluR2 and mGluR8 (IC50 >10 μM) 1. FITM demonstrates antipsychotic-like effects in several animal models.1 The radiolabeled version [18F]FITM was successfully profiled as a PET ligand for mGluR1 imaging in rat and monkey brain2.
Scientific background
FITM is a potent and selective antagonist of mGluR1, displaying an IC50 value of 5.1 nM1 with little inhibition of mGluR2, mGluR5, and mGluR81,2.Glutamate is the most abundant excitatory neurotransmitter in the central nervous system and it modulates activity of many types of synapses by activating in part metabotropic glutamate receptors (mGluRs), members of G-protein coupled receptors (GPCRs). These receptors are divided into three groups based on sequence homology with a total of eight subtypes, mGluR1 to mGluR8.mGluR1 plays an important role in the central sensitization of pain and in a variety of functions with potential implications in neurological and psychiatric disorders2,3.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
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