| Identification | Back Directory | [Name]
LY2794193 | [CAS]
2173037-97-1 | [Synonyms]
LY2794193
Bicyclo[3.1.0]hexane-2,6-dicarboxylic acid, 2-amino-4-[(3-methoxybenzoyl)amino]-, (1S,2S,4S,5R,6S)- | [Molecular Formula]
C16H18N2O6 | [MOL File]
2173037-97-1.mol | [Molecular Weight]
334.32 |
| Chemical Properties | Back Directory | [Boiling point ]
598.6±50.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
1.78±0.60(Predicted) | [color ]
White to off-white | [Water Solubility ]
Water : 2 mg/mL (5.98 mM; ultrasonic and adjust pH to 14 with NaOH) |
| Hazard Information | Back Directory | [Uses]
LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM，EC50=0.47 nM; hmGlu2 Ki=412 nM，EC50=47.5 nM)[1]. | [Biological Activity]
LY2794193 is a potent and selective mGlu3 receptor agonist (hmGlu3 Ki=0.927 nM, EC50=0.47 nM; hmGlu2 Ki=412 nM, EC50=47.5 nM). | [in vitro]
LY2794193 exhihits inhibition of spontaneous Ca 2+ oscillations in cultured rat cortical neurons with an EC 50 of 43.6 nM.
In the rat cortical neuron Ca 2+ oscillation assay, LY2794193 exhibits a biphasic inhibition of spontaneous Ca 2+ transients (high affinity EC 50 =0.44 nM; 48% of the total agonist response; low affinity EC 50 =43.6 nM; 52% of the total agonist response) with combined maximal agonist efficacy (E max ) of 66%. < /p> | [in vivo]
LY2794193 (1-30 mg/kg, sc), given 30 min prior to PCP (5 mg/kg, sc) leads a dose-related reduction in ambulations.
LY2794193 (1 mg/ kg; iv) exhibits moderate clearance (18.3 mL/min per kg) and volume of distribution (1.17 L/kg) with a calculated plasma half-life (T 1/2 ) of 3.1 h in Male Sprague-Dawley rats.
LY2794193 (3 mg/kg; sc) leads to the rapid appearance in the plasma (AUC=9.9 μM; C max =6.78 μM; T max =0.44 h) and a calculated bioavailability of 121% in male Sprague-Dawley rats. | Animal Model: | Male Sprague-Dawley rats | | Dosage: | 1, 3, 10, or 30 mg/kg < /td> | | Administration: | Administrated sc; given 30 min prior to PCP (5 mg/kg, sc) | | Result: | A dose-related reduction in ambulations was observed, with the 10 and 30 mg/kg dose groups found to be statistically significant. | < /tr> | [target]
| mGluR3 0.47 nM (EC 50 ) | mGluR3 0.927 nM (Ki) | mGluR2 47.5 (EC 50 ) | mGluR2 412 (Ki) | | [IC 50]
mGluR3: 0.47 nM (EC50); mGluR3: 0.927 nM (Ki); mGluR2: 47.5 (EC50); mGluR2: 412 (Ki) | [References]
[1] Monn JA, et al. Synthesis and Pharmacological Characterization of C4β-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4 S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid ( DOI:10.1021/acs.jmedchem.7b01481 |
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