138000
D-Amino Acid Oxidase Inhibitor
4H-Thieno[3,2-b]pyrrole-5-carboxylic acid, D-AAO Inhibitor, Compound 8
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Telefon: +49 6151 72-0
Fax: +49 6151 72 2000
31 Mai 2012
wird geladen
A cell-permeable thienopyrrole compound that potently inhibits the cellular activity of transfected D-amino acid oxidase (DAO/DAAO/DAMOX/OXDA) in CHO cells (IC50 against human and rat DAO = 145 and 114 nM, respectively), while exhibiting no activity towards D-aspartate oxidase (DDO; IC50 >5 µM), P450 enzymes CYP3A4/2D6/3C9 (IC50 >10 µM), and a panel of over 150 other enzymes, receptors, and ion channels. Although in vivo treatment of Compound 8 (200 mg/kg, i.p.) is shown to effectively inhibit DAO activity in rat brain and kidney (by 96% and 80%, respectively), the resulting D-serine concentration increase in the periphery and central nervous system appears to be far from sufficient to produce adequate antipsychotic and cognitive enhancing effects.
| Produktinformationen | |||
|---|---|---|---|
| Form | Beige solid | ||
| Protect from Light | Ja | ||
| Packaged under inert gas | Ja | ||
| Purity | ≥97% by HPLC | ||
| Chemische Formel | C7H5NO2S | ||
| CAS-Nummer | 39793-31-2 | ||
| Lager- und Versandinformationen | |||
|---|---|---|---|
| Lagerkategorie | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Harmful |
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| Sicherheitshinweise | |||
|---|---|---|---|
| S-Satz |
S: 26-36/37/39 |
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| R-Satz |
R: 22-36/37/38 |
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