产品名称

英文名称：LY404039

同义词

635318-11-5、LY404039、Pomaglumetad、LY-404039、(1R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide、LY 404039、531QUG7P9E、CHEMBL375611、LY-404039, (-)-、UNII-531QUG7P9E、MFCD11974011、SCHEMBL1088010、CHEBI94640、DTXSID40212943、BCPP000

产品性质

CAS编号：635318-11-5

分子式：C7H9NO6S

分子量：235.21

PubChem编号：9834591

英文别名：635318-11-5|LY404039|Pomaglumetad|LY-404039|(1R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide|LY 404039|531QUG7P9E|CHEMBL375611|LY-404039, (-)-|UNII-531QUG7P9E|MFCD11974011|SCHEMBL1088010|CHEBI94640|DTXSID40212943|BCPP000

规格或纯度：98%

英文名称：LY404039

生化机理：Description IC50 Value149nM(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

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍LY404039 是一种有效的，选择性的，具有口服活性的 mGluR2 和 mGluR3 激动剂，对重组人 mGluR2 和 mGluR3 的 Ki 分别为 149 nM 和 92 nM，比对其他受体/转运蛋白的抑制性高 100 倍以上。LY404039 具有抗精神病和抗焦虑的作用。

ALogP：-4.8

IUPAC Name：(1R,4S,5S,6S)-4-amino-2,2-dioxo-2λ6-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid

INCHI：InChI=1S/C7H9NO6S/c8-7(6(11)12)1-15(13,14)4-2(3(4)7)5(9)10/h2-4H,1,8H2,(H,9,10)(H,11,12)/t2-,3-,4+,7+/m1/s1

InChi Key：AVDUGNCTZRCAHH-MDASVERJSA-N

Canonical SMILES：C1C(C2C(C2S1(=O)=O)C(=O)O)(C(=O)O)N

Isomeric SMILES：C1[C@]([C@@H]2[C@H]([C@@H]2S1(=O)=O)C(=O)O)(C(=O)O)N

PubChem CID：9834591

溶解性：DMSO 1 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

产品包装