LY2794193
LY2794193 性质
| 沸点 | 598.6±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.50±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 形态 | 固体 |
| 酸度系数(pKa) | 1.78±0.60(Predicted) |
| 颜色 | 白色至米白色 |
| 水溶解性 | Water : 2 mg/mL (5.98 mM; ultrasonic and adjust pH to 14 with NaOH) |
LY2794193 用途与合成方法
|
mGluR3 0.47 nM (EC 50 ) |
mGluR3 0.927 nM (Ki) |
mGluR2 47.5 (EC 50 ) |
mGluR2 412 (Ki) |
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%.
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.
| Animal Model: | Male Sprague-Dawley rats |
| Dosage: | 1, 3, 10, or 30 mg/kg |
| Administration: | Administrated s.c.; given 30 min prior to PCP (5 mg/kg, s.c.) |
| Result: | A dose-related reduction in ambulations was observed, with the 10 and 30 mg/kg dose groups found to be statistically significant. |
LY2794193 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025-12-22 | HY-119243 | 2173037-97-1 | 1 mg | 1980 | |
| 2025-12-22 | HY-119243 | LY2794193 | 2173037-97-1 | 10 mM * 1 mLin DMSO | 3641 |
