(1R,4S,5S,6S)-4-AMINO-2-THIABICYCLO 3.1.0 HEXANE-4,6-DICARBOXYLIC ACID 2,2-DIOXIDE (LY 404039)
2-Thiabicyclo[3.1.0]hexane-4,6-dicarboxylicacid, 4-amino-, 2,2-dioxide, (1R,4S,5S,6S)-
CAS: 635318-11-5
Molecular Formula: C7H9NO6S
(1R,4S,5S,6S)-4-AMINO-2-THIABICYCLO 3.1.0 HEXANE-4,6-DICARBOXYLIC ACID 2,2-DIOXIDE (LY 404039) - Names and Identifiers
(1R,4S,5S,6S)-4-AMINO-2-THIABICYCLO 3.1.0 HEXANE-4,6-DICARBOXYLIC ACID 2,2-DIOXIDE (LY 404039) - Physico-chemical Properties
| Molecular Formula | C7H9NO6S |
| Molar Mass | 235.21 |
| Density | 1.888 |
| Melting Point | >250 °C(Solv: water (7732-18-5)) |
| Boling Point | 600.3±55.0 °C(Predicted) |
| pKa | 1.15±0.40(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | LY404039 efficiently activated recombinant human mGlu2, mGlu3 receptors and mGlu2/3 receptors expressed by murine neurons with K I of 149, 92 and 88nm, respectively. LY404039 has a low affinity for Type III mGlu receptors (including mGlu6, mGlu7 and mGlu8), with K I values greater than 5 μm. LY404039 also has little affinity for ionotropic glutamate receptors, glutamate transporter subtypes, monoamines, and other receptors. In cells expressing human mGlu2 and mGlu3 receptors, LY404039 potently inhibited forskolin-stimulated cAMP formation. LY404039 blocks electrically evoked excitatory activity in the striatum and blocks serotonin-induced L-glutamate release in the prefrontal cortex. In the limbic and forebrain regions associated with psychosis, LY404039 can modulate glutamatergic activity, LY404039 has no side effects, anxiolytic and antipsychotic. LY404039 showed higher plasma exposure and better oral bioavailability. LY404039 is valuable in the treatment of psychopathology, including anxiety and confusion. |
| In vivo study | In mGlu2 and mGlu2/3 receptor-deficient mice, LY404039 had no antipsychotic effect on PCP and AMP-induced behavior, but the opposite was true in mGlu3 receptor-deficient mice. However, in contrast to LY404039, clozapine and risperidone inhibited PCP-induced behavior in both wild-type and mglu 2/3 receptor-deficient mice. LY404039 reduces response to EtOH in Pavlov's natural recovery test (PSR). LY404039 also reduced the expression of alcohol deprivation effects (ADE), but did not reduce the response to EtOH. LY404039 inhibits the expression of alcohol exploration and relapse behavior without altering alcohol self-control behavior. LY404039 reduces amphetamine and phencyclidine-induced rapid locomotions. LY404039 can inhibit the conditioned avoidance response can also reduce the strong fear of fear in rats. Importantly, LY404039 does not produce sedative effects and mechanical damage when applied to the conditioned avoidance task. When LY40403 acts on the prefrontal cortex, it also enhances the release/flow of dopamine and serotonin. |
(1R,4S,5S,6S)-4-AMINO-2-THIABICYCLO 3.1.0 HEXANE-4,6-DICARBOXYLIC ACID 2,2-DIOXIDE (LY 404039) - Preparation solution concentration reference
| 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 |
| 5 mM | 0.085 ml | 0.425 ml | 0.85 ml |
Last Update：2024-01-02 23:10:35
(1R,4S,5S,6S)-4-AMINO-2-THIABICYCLO 3.1.0 HEXANE-4,6-DICARBOXYLIC ACID 2,2-DIOXIDE (LY 404039) - Reference Information
| biological activity | LY404039 is a potent recombinant human mGlu2/mGlu3 receptor agonist, ki is 149 nM/92 nM, which is more than 100 times higher than that of other glutamate receptors, glutamate transporters and other receptors. Phase 3. |
| Target | Value |
| Rat neurons expressing native mGlu2/3 | 88 nM(Ki) |
| Recombinant human mGlu3 | 92 nM(Ki) |
| Recombinant human mGlu2 | 149 nM(Ki) |
Last Update：2024-04-09 02:00:10
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Product Name: (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 Visit Supplier Webpage Request for quotation
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