| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Up to 10 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 2-cyclopropyl-5-[1-(2-fluoropyridin-3-yl)-5-methyltriazol-4-yl]-3H-isoindol-1-one.
- CAS number: 864864-17-5
- Molecular formula: C19H16FN5O.
- Purity: >96%
- Concentration: 10 nM - 10 µM.
- Form: Lyophilized powder.
- Solubility: Up to 10 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
- Reconstitution: Up to 10 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
- 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: CFMTI is a selective and potent allosteric antagonist of mGluR1 receptors. It inhibits L-glutamate-induced intracellular Ca2+ mobilization in CHO cells expressing human and rat mGluR1a with IC50 values of 2.6 and 2.3 nM, respectively. It is highly selective for mGluR1 over mGluR5 (2000-fold), and does not affect mGluR subtypes and other receptors at 10 µM1.
Scientific background
CFMTI is a negative allosteric modulator of mGluR1 receptors with IC50 values of 2.6 and 2.3 nM for human and rat mGluR1 expressed in CHO cells, respectively. CFMTI demonstrates high potency and selectivity for the receptor both in vitro and in vivo after oral administration and shows very low potency for other mGluR subtypes1,2.Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCRs) that play an important role in synaptic plasticity and other neuro-physiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly expressed on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells and neural stem cells and the formation of the hippocampus3.
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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