货号	品牌	包装	目录价	您的价格
L127760-5mg	阿拉丁	5mg	¥340.90	请登录
L127760-25mg	阿拉丁	25mg	¥1111.90	请登录
L127760-50mg	阿拉丁	50mg	¥1976.90	请登录
L127760-10mg	阿拉丁	10mg	¥610.90	请登录
L127760-100mg	阿拉丁	100mg	¥3161.90	请登录

产品名称	LY404039
中文名称	LY404039
CAS号	635318-11-5
分子式（M.F.）	C7H9NO6S
分子量（M.W.）	235.21
储存条件	-20°C储存

溶解性	DMSO 1 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
存贮条件	储存温度-20°C
备注	LY404039 is a potent agonist of recombinant human mGlu2/mGlu3 receptors with Ki of 149 nM/92 nM, shows >100-fold selectivity over ionotropic glutamate receptors, glutamate transporters, and other receptors. Phase 3.
生化机理	Description: IC50 Value:149nM(Ki for mGlu2);92nM(Ki for mGlu3)[1] LY404039 is a inhibitor for mGlu1 and mGlu2, which can also inhibit dopamine receptor[2].Metabotropic glutamate (mGlu) receptors have been shown to mediate a number of behaviors including emotionality and responsivity to stress as demonstrated by efficacy in preclinical and clinical studies. in vitro: Similar to LY354740, LY404039 is a nanomolar potent agonist at recombinant human mGlu2 and mGlu3 receptors (K(i) = 149 and 92, respectively) and in rat neurons expressing native mGlu2/3 receptors (Ki = 88). LY404039 is highly selective for mGlu2/3 receptors, showing more than 100-fold selectivity for these receptors, versus ionotropic glutamate receptors, glutamate transporters, and other receptors targeted by known anxiolytic and antipsychotic medications[1]. in vivo: LY404039 attenuated amphetamine- and phencyclidine-induced hyperlocomotion (3-30 and 10 mg/kg, respectively). LY404039 (3-10 mg/kg) inhibited conditioned avoidance responding. LY404039 also reduced fear-potentiated startle in rats (3-30 microg/kg) and marble burying in mice (3-10 mg/kg), indicating anxiolytic-like effects. Importantly, LY404039 did not produce sedative effects or motor impairment as measured by rotarod performance and lack of escape failures in the conditioned avoidance task (at doses up to 30 and 10 mg/kg, respectively). LY404039 (10 mg/kg) also increased dopamine and serotonin release/turnover in the prefrontal cortex [3]. Clinical trial: An Absolute Bioavailability Study of LY-2140023 and LY-404039 in Healthy Subjects Using the Intravenous Tracer Method. Phage1
别名	(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;(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

LY404039

LY404039 （订货以英文为准）