化合物 T15807 T15807

Product Introduction
Bioactivity


英文名: LY2794193

描述: 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).

体外活性: 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%.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 2 mg/mL (5.98 mM)


关键字: LY 2794193 | LY-2794193 | LY2794193

相关产品: KGA-2727 | Ertugliflozin | Remogliflozin etabonate | Mizagliflozin | HSK0935 | Empagliflozin | Canagliflozin | Licogliflozin | Canagliflozin hemihydrate | SGLT inhibitor-1

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