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LY404039

    
≥98%

(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

源葉(MedMol)
S80853 一鍵復(fù)制產(chǎn)品信息
635318-11-5
C7H9NO6S
235.21
貨號(hào) 規(guī)格 價(jià)格 上海 北京 武漢 南京 購(gòu)買(mǎi)數(shù)量
S80853-5mg
≥98% ¥340.00 5 - - -
S80853-10mg
≥98% ¥610.00 4 - - -
S80853-25mg
≥98% ¥1111.00 3 - - -
S80853-50mg
≥98% ¥1970.00 2 - - -
S80853-100mg
≥98% ¥3161.00 1 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(shū)(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

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

產(chǎn)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
靶點(diǎn): mGlu2 Receptor:149 nM (Ki, Recombinant human mGluR2);hmGluR3:92 nM (Ki);GlucocorticoidReceptor;GluR
體內(nèi)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
參考文獻(xiàn): 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
保存條件: -20℃
配置溶液濃度參考:
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: 部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。

參考文獻(xiàn)

質(zhì)檢證書(shū)(COA)

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批號(hào):JS298415 貨號(hào):S20001-25g
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摩爾濃度計(jì)算器

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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