货号	规格	价格	上海	北京	珠海	重庆	武汉
S80853-5mg促销	≥98%	￥340.00 ￥306.00 S80853-5mg ￥306.00 现货	5 5	-	-	-	-
S80853-10mg促销	≥98%	￥610.00 ￥549.00 S80853-10mg ￥549.00 现货	4 4	-	-	-	-
S80853-25mg促销	≥98%	￥1110.00 ￥1000.00 S80853-25mg ￥1000.00 现货	3 3	-	-	-	-
S80853-50mg促销	≥98%	￥1970.00 ￥1770.00 S80853-50mg ￥1770.00 现货	2 2	-	-	-	-
S80853-100mg促销	≥98%	￥3160.00 ￥2840.00 S80853-100mg ￥2840.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with Kis of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects

靶点：

mGlu2 Receptor:149 nM (Ki, Recombinant human mGluR2);hmGluR3:92 nM (Ki);GlucocorticoidReceptor;GluR

体内研究：

LY404039 attenuates amphetamine- and phencyclidine-induced hyperlocomotion (3-30 and 10 mg/kg, respectively). LY404039 (3-10 mg/kg) inhibits conditioned avoidance responding. LY404039 also reduces fear-potentiated startle in rats (3-30 μg/kg) and marble burying in mice (3-10 mg/kg), indicating anxiolytic-like effects. LY404039 (10 mg/kg) also increases dopamine and serotonin release/turnover in the prefrontal cortex. Following oral administration of LY404039 to fasted rats at doses of 1, 3, or 10 mg/kg, exposure increased proportionally with dose. LY404039 (10 mg/kg; p.o.) treatment shows the Cmax is 1528.5 ng/mL and Tmax is 2 hours in rats

参考文献：

1. Linda M Rorick-Kehn, et al. Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]- 2. Seeman P. An agonist at glutamate and dopamine D2 receptors, LY404039. Neuropharmacology. 2013 Mar;66:87-8. [Content Brief] 3. Rorick-Kehn LM, et al. In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonistLY404039 in animal models of psychiatric disorders. Psychopharmacology (Berl). 2007 Jul;193(1):121-36.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	4.252 ml	21.258 ml	42.515 ml
5 mM	0.85 ml	4.252 ml	8.503 ml
10 mM	0.425 ml	2.126 ml	4.252 ml
50 mM	0.085 ml	0.425 ml	0.85 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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LY404039

(1R,4S,5S,6S)-4-[[(2S)-2-Amino-4-(methylthio)-1-oxobutyl]amino]-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)