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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 Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $523 | 10-14 weeks | |
25 mg | $1,810 | 10-14 weeks | |
50 mg | $2,360 | 10-14 weeks | |
100 mg | $3,270 | 10-14 weeks |
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. |
Molecular Weight | 334.32 |
Formula | C16H18N2O6 |
Cas No. | 2173037-97-1 |
Relative Density. | 1.50 g/cm3 (Predicted) |
Storage | Powder: -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
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