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LY404039
产品别名
635318-11-5
LY404039
(–)-(1R,4S,5S,6S)-4-Amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid
LY 404039
LY-404039
LY-404,039
(1R,4S,5S,6S)-4-Amino-2-thiabicyclo[3.1.0]hexane-4,6-dicarboxylic acid 2,2-dioxide
结构式
基本信息
Empirical Formula【经验(实验)分子式】 | C7H9NO6S |
Molecular weight | 235.21 |
MDL number | MFCD11974011 |
Biochem/physiol Actions【生化/生理作用】 | LY404039 is a potent and selective group II metabotropic glutamate receptors mGluR2/3 agonist (Ki = 15 nM against against [3H]LY341495 for binding rat neurons; Ki = 149 nM and 92 nM, respectively, using membrane from human mGluR2- or mGluR3-expressing cells) with >100-fold selectivity over 16 other receptors/transproters, including iGluRs and EAAT1/2/3. LY404039 inhibits forskolin-stimulated c-AMP production in RGT cells expressing human mGluR2 (EC50 = 23 nM) or mGluR3 (EC50 = 48 nM) with little or no potency toward mGluR1a/5a/4a/6/7a/8a-expressing cells (EC50 >10 μM). LY404039 is orally available (Cmax 1528.5 ng/mL, Tmax 2 h; 10 mg/kg p.o. in rats) and exhibits antipsychotic and anxiolytic efficacy in rats (3-30 mg/kg) in vivo. |
产品性质
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | powder |
optical activity【旋光性】 | [α]/D -69 to -79°, c = 1.0 in 1 M NaOH |
color【颜色】 | white to gray |
solubility【溶解性】 | DMSO: 2 mg/mL, clear (warmed) |
storage temp.【储存温度】 | −20℃ |
SMILES string | [H][C@]1([C@@](C(O)=O)(N)C2)[C@@]([C@@H]1C(O)=O)([H])S2(=O)=O |
安全信息
Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
WGK | WGK 3 |