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LY2794193

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Catalog No. T15807Cas No. 2173037-97-1
Alias LY 2794193

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.

LY2794193

LY2794193

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Purity: 98.15%
Catalog No. T15807Alias LY 2794193Cas No. 2173037-97-1
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.
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5 mg$1,399-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.15%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
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]
SynonymsLY 2794193
Chemical Properties
Molecular Weight334.32
FormulaC16H18N2O6
Cas No.2173037-97-1
SmilesC(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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM2.9911 mL14.9557 mL29.9115 mL149.5573 mL
DMSO
1mg5mg10mg50mg
5 mM0.5982 mL2.9911 mL5.9823 mL29.9115 mL
10 mM0.2991 mL1.4956 mL2.9911 mL14.9557 mL
20 mM0.1496 mL0.7478 mL1.4956 mL7.4779 mL
50 mM0.0598 mL0.2991 mL0.5982 mL2.9911 mL
100 mM0.0299 mL0.1496 mL0.2991 mL1.4956 mL

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TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
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Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

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