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LY2794193

Catalog No. T15807Cas No. 2173037-97-1

LY2794193 is a highly effective and selective agonist of the mGlu3 receptor (hmGlu3 Ki=0.927 nM,EC50=0.47 nM; hmGlu2 Ki=412 nM,EC50=47.5 nM).

LY2794193

LY2794193

Catalog No. T15807Cas No. 2173037-97-1
LY2794193 is a highly effective and selective agonist of the mGlu3 receptor (hmGlu3 Ki=0.927 nM,EC50=0.47 nM; hmGlu2 Ki=412 nM,EC50=47.5 nM).
Pack SizePriceAvailabilityQuantity
5 mg$52310-14 weeks
25 mg$1,81010-14 weeks
50 mg$2,36010-14 weeks
100 mg$3,27010-14 weeks
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Product Introduction

Bioactivity
Description
LY2794193 is a highly effective and selective agonist of the mGlu3 receptor (hmGlu3 Ki=0.927 nM,EC50=0.47 nM; hmGlu2 Ki=412 nM,EC50=47.5 nM).
Targets&IC50
mGluR2:412 (ki), mGluR2:47.5 (EC50), mGluR3:0.47 nM (EC50), mGluR3:0.927 nM (ki)
In vitro
LY2794193 shows inhibition of spontaneous Ca2+ oscillations in cultured rat cortical neurons (EC50: 43.6 nM). LY2794193 shows a biphasic inhibition of spontaneous Ca2+ transients (high-affinity EC50=0.44 nM; 48% of the total agonist response; low-affinity EC50=43.6 nM; 52% of the total agonist response), in the rat cortical neuron Ca2+ oscillation assay, with combined maximal agonist efficacy (Emax) of 66%.
In vivo
LY2794193 (1 mg/kg; i.v.) displays moderate clearance (18.3 mL/min per kg) and volume of distribution (1.17 L/kg) with a calculated plasma half-life (T1/2) of 3.1 h in Male Sprague-Dawley rats. LY2794193 (3 mg/kg; s.c.) leads to the rapid appearance in the plasma (AUC=9.9 μM; Cmax=6.78 μM; Tmax=0.44 h) and a calculated bioavailability of 121% in male Sprague-Dawley rats. LY2794193 (1-30 mg/kg, s.c.), given 30 min prior to PCP (5 mg/kg, s.c.) leads a dose-related reduction in ambulations.
Chemical Properties
Molecular Weight334.32
FormulaC16H18N2O6
Cas No.2173037-97-1
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: 2 mg/mL (5.98 mM), when pH is adjusted to 14 with NaOH. Sonication is recommended.
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM2.9911 mL14.9557 mL29.9115 mL149.5573 mL
5 mM0.5982 mL2.9911 mL5.9823 mL29.9115 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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