| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: 5-[1-(2,4-difluorophenyl)-5-methyltriazol-4-yl]-2-propan-2-yl-3H-isoindol-1-one.
- Also known as: DFMTI
- PubChem CID: 15985251
- Molecular formula: C20H18F2N4O.
- Purity: >98%
- Concentration: 10 nM - 10 µM.
- Form: Lyophilized powder.
- Solubility: Up to 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
- Reconstitution: Up to 25 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 receptor
- Source: Synthetic
- Activity: MK-5435 is a potent and selective allosteric mGluR1 antagonist, inhibiting human and rat mGluR1 with IC50 of 4.3 and 3.6 nM, respectively. It is selective over mGluR5 (IC50 = 1.5 µM), mGluR2 and mGluR8 (IC50 = 10 µM), and has no affinity for the quisqualic binding site (IC50 >10 µM). in vivo, following an oral dose of 1 mg/kg, plasma and brain concentrations in mice were 0.17 µM and 0.45 nmol/g respectively, at 30 min post-dose1.
- Alternative names: DFMTI
Scientific background
MK-5435 is an allosteric negative modulator of mGluR1 receptors. This synthetic compound demonstrates high potency and selective antagonistic activities towards the receptor with IC50 values of 4.3 + 1.3 nM1.Metabotropic glutamate receptors (mGluRs) are G protein coupled receptors (GPCR) 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 found on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells and neural stem cell and the formation of the hippocampus2.
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
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