mGluR5 modulator 1
mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 1261171-52-1
- Fòrmula: C18H19ClFN3O2
- Peso molecular:363.81
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
IC50 & Target
mGluR5[1]
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.6 μM
Compound: 2c
|
Positive allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as Ca2+ influx by FLIPR assay
Positive allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as Ca2+ influx by FLIPR assay
|
[PMID: 21067920] |
In Vitro
mGluR5 modulator 1 (compound 2c; 0.1-0.00001 nM) potentiates the L-glutamate and DHPG responses to the same maximum response as the orthosteric agonists alone in the Ca2+ mobilization and IP1 accumulation assays[1].
mGluR5 modulator 1 (0.1-0.00001 nM) potentiates the L-glutamate and DHPG responses above the orthosteric agonist maximal response in the ERK1/2 phosphorylation assay[1].
mGluR5 modulator 1 induces mGlu5 internalization in the absence of add orthosteric agonist or antagonist[1].
mGluR5 modulator 1 potentiates the responses induced by both orthosteric agonists (L-glutamate or DHPG) in Ca2+ mobilization (pKB=5.4 and 5.3, respecyively), inositol monophosphate accumulation, and ERK1/2 phosphorylation signaling (pKB=5.88 and 5.4, respecyively) assays in HEK293A-mGlu5-low cells[1].
mGluR5 modulator 1 enhances the effect of DHPG in cortical neurons with pEC50 values of 6.32 and 6.33 in Ca2+ mobilization and inositol monophosphate (IP1) accumulation assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 1261171-52-1
-
Peso molecular 363.81
-
Fòrmula C18H19ClFN3O2
-
SMILES
FC1=CC(Cl)=CC=C1N2CCN(C(COCC3=CC=NC=C3)=O)CC2
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)