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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 | Availability | Quantity |
---|---|---|---|
5 mg | $523 | In Stock | |
25 mg | $1,810 | 10-14 weeks | |
50 mg | $2,360 | 10-14 weeks | |
100 mg | $3,270 | 10-14 weeks |
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 | mGluR2:412 (ki), mGluR3:0.927 nM (ki), mGluR3:0.47 nM (EC50), 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] |
Alias | 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. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 1 mg/mL (2.99 mM), adjust pH to 14 with NaOH DMSO: 180 mg/mL (538.41 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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