LY2794193

• CAT Number: I019313
• CAS Number: 2173037-97-1
• Molecular Formula: C16H18N2O6
• Molecular Weight: 334.32
• Purity: ≥95%
• Synonyms: (1S,2S,4S,5R,6S)-2-amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic acid
• InChI: InChI=1S/C16H18N2O6/c1-24-8-4-2-3-7(5-8)13(19)18-9-6-16(17,15(22)23)12-10(9)11(12)14(20)21/h2-5,9-12H,6,17H2,1H3,(H,18,19)(H,20,21)(H,22,23)/t9-,10-,11-,12-,16-/m0/s1
• InChIKey: UXNRHIJPZNNDDJ-VZAVHYRXSA-N
• SMILES: COC1=CC=CC(=C1)C(=O)NC2CC(C3C2C3C(=O)O)(C(=O)O)N

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].
LY2794193 exhihits inhibition of spontaneous Ca2+ oscillations in cultured rat cortical neurons with an EC50 of 43.6 nM[1].
In the rat cortical neuron Ca2+ oscillation assay, LY2794193 exhibits 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) with combined maximal agonist efficacy (Emax) of 66%[1].
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[1].
LY2794193 (1 mg/kg; i.v.) exhibits 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[1].
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[1].

Reference

[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 (
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