LY2794193  ≥98%

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包装规格:1mg 5mg in glass bottle
溶解性:溶于DMSO(3mg/mL超声)
产品描述:基本信息 产品编号: L11028 产品名称: LY2794193 CAS: 2173037-97-1   储存条件 粉末 -20℃ 四年     分子式: C16H18N2O6 溶于液体 -80℃ 6个月 分子量: 334.32 -20℃ 1个月 化学名:  (1S,2S,4S,5R,6S)-2-Amino-4-[(3-methoxybenzene-1-carbonyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic acid Solubility (25°C):   体外:   DMSO   Ethanol   Water   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.9911mL 14.9557mL 29.9115mL 5mM 0.5982mL 2.9911mL 5.9823mL   生物活性 产品描述 一种高效的选择性 mGlu3 受体激动剂。 靶点 mGluR3 0.47nM (EC50) mGluR3 0.927nM (Ki) mGluR2 47.5 (EC50) mGluR2 412 (Ki)   体外研究 LY2794193 exhihits inhibition of spontaneous Ca2+oscillations in cultured rat cortical neurons with an EC50 of 43.6nM.In the rat cortical neuron Ca2+oscillation assay,LY2794193 exhibits a biphasic inhibition of spontaneous Ca2+transients (high affinity EC50=0.44nM;48% of the total agonist response;low affinity EC50=43.6nM;52% of the total agonist response) with combined maximal agonist efficacy (Emax) of 66%. 体内研究 LY2794193 (1-30mg/kg,s.c.),given 30 min prior to PCP (5mg/kg,s.c.) leads a dose-related reduction in ambulations.LY2794193 (1mg/kg;i.v.) exhibits moderate clearance (18.3mL/min per kg) and volume of distribution (1.17L/kg) with a calculated plasma half-life (T1/2) of 3.1 h in Male Sprague-Dawley rats.LY2794193 (3mg/kg;s.c.) leads to the rapid appearance in the plasma (AUC=9.9μM;Cmax=6.78μM;Tmax=0.44h) and a calculated bioavailability of 121% in male Sprague-Dawley rats. Animal Model: Male Sprague-Dawley rats Dosage: 1,3,10,or 30mg/kg Administration: Administrated s.c.;given 30 min prior to PCP (5mg/kg,s.c.) Result: A dose-related reduction in ambulations was observed,with the 10 and 30mg/kg dose groups found to be statistically significant.
保存条件:-20℃