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LY2794193, a potent and selective mGlu3 (metabotropic glutamate 3) receptor agonist, Ki=0.927 nM, EC50=0.47 nM, reduces akathisia seizures and depressive-like behaviors and increases GAT1, GLAST and GLT-1 protein levels in rats.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $1,399 | - | In Stock |
| Description | LY2794193, a potent and selective mGlu3 (metabotropic glutamate 3) receptor agonist, Ki=0.927 nM, EC50=0.47 nM, reduces akathisia seizures and depressive-like behaviors and increases GAT1, GLAST and GLT-1 protein levels in rats. |
| Targets&IC50 | mGluR3:0.47 nM (EC50), mGluR2:412 (ki), mGluR3:0.927 nM (ki), mGluR2:47.5 (EC50) |
| In vitro | When its agonist responses were examined in cells co-expressing a promiscuous G protein (Gαq), LY2794193 exhibited agonist activity against both hmGlu3 (EC50 value of 11.6 nM) and hmGlu2 (EC50 value of 277 nM).[1] |
| In vivo | Methods: Two doses of LY2794193 (0.1, 0.3, and 1 mg/kg, sc) and LY2794193 (1, 3, and 10 mg/kg, sc) were administered to rats; the first study employed dose levels, while the second evaluated higher doses; in each study, plasma and cerebrospinal fluid (CSF) levels were determined 1 h after LY2794193 administration. Results: Plasma and CSF levels of LY2794193 were observed at all dose levels, and a linear increase in each compartment with increasing dose was observed. The fraction of LY2794193 partitioning into the CSF was both low and highly consistent across dose levels, with a CSF to plasma ratio of 1% calculated over a 100-fold concentration range. [1] |
| Synonyms | LY 2794193 |
| Molecular Weight | 334.32 |
| Formula | C16H18N2O6 |
| Cas No. | 2173037-97-1 |
| Smiles | C(O)(=O)[C@H]1[C@]2([C@@]1([C@@](C(O)=O)(N)C[C@@H]2NC(=O)C3=CC(OC)=CC=C3)[H])[H] |
| Relative Density. | 1.50 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: 1 mg/mL (2.99 mM), when pH is adjusted to 14 with NaOH. DMSO: 180 mg/mL (538.41 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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