LY2794193 是一种高效的选择性 mGlu3 受体激动剂 (hmGlu3 K_i=0.927 nM，EC₅₀=0.47 nM; hmGlu2 K_i=412 nM，EC₅₀=47.5 nM)。

LY2794193 is a highly potent and selective mGlu3 receptor agonist (hmGlu3 K i =0.927 nM，EC 50 =0.47 nM; hmGlu2 K i =412 nM，EC 50 =47.5 nM).

Solid

mGluR3 0.47 nM (EC50) mGluR3 0.927 nM (Ki)

LY2794193 exhihits inhibition of spontaneous Ca oscillations in cultured rat cortical neurons with an EC50 of 43.6 nM.
In the rat cortical neuron Ca oscillation assay, LY2794193 exhibits a biphasic inhibition of spontaneous Ca 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%. has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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 (T 1/2 ) 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; C max =6.78 μM; T max =0.44 h) and a calculated bioavailability of 121% in male Sprague-Dawley rats. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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 (

In Vitro: DMSO : 200 mg/mL (598.23 mM; Need ultrasonic)H₂O : 2 mg/mL (5.98 mM; ultrasonic and adjust pH to 14 with NaOH)配制储备液