nur für Forschungszwecke
Kat.-Nr.S2302
| Verwandte Ziele | HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite |
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| Weitere Dehydrogenase Inhibitoren | Vorasidenib (AG-881) (R)-GNE-140 CPI-613 (Devimistat) Sodium Dichloroacetate (DCA) AGI-5198 Gossypol Acetate AGI-6780 Emodin NCT-503 Brequinar |
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | PMID |
|---|---|---|---|---|---|---|
| HEK293 | Function assay | Inhibition of human microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay, IC50=0.001μM. | 19564108 | |||
| HEK293 | Function assay | Inhibition of mouse microsomal 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay, IC50=0.008μM. | 19564108 | |||
| HEK293 | Function assay | Inhibition of human microsomal 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay, IC50=0.01μM. | 19564108 | |||
| HEK293 | Function assay | Inhibition of mouse liver microsome 11betaHSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay, IC50=0.015μM. | 19574056 | |||
| HEK293 | Function assay | Inhibition of human 11beta-HSD2 expressed in human HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay, IC50=0.0007μM. | 22148241 | |||
| HEK293 | Function assay | Inhibition of human 11beta-HSD1 expressed in human HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay, IC50=0.0186μM. | 22148241 | |||
| HEK293 | Function assay | Inhibition of mouse 11beta-HSD1 expressed in human HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay, IC50=0.0295μM. | 22148241 | |||
| HEK293 | Function assay | Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay, IC50=0.0004μM. | 22360639 | |||
| HEK293 | Function assay | Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay, IC50=0.003μM. | 22360639 | |||
| HEK293 | Function assay | Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay, IC50=0.006μM. | 22360639 | |||
| HEK293 | Function assay | 60 mins | Inhibition of human 11beta-HSD2 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA, EC50=0.001μM. | 22440625 | ||
| HEK293 | Function assay | 60 mins | Inhibition of mouse 11beta-HSD1 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA, EC50=0.008μM. | 22440625 | ||
| HEK293 | Function assay | 60 mins | Inhibition of human 11beta-HSD1 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA, EC50=0.01μM. | 22440625 | ||
| MDCK | Cytotoxicity assay | 48 hrs | Cytotoxicity against MDCK cells assessed as reduction in cell viability after 48 hrs by MTT assay, EC50=15.2μM. | 25801933 | ||
| MDCK | Antiviral assay | Antiviral activity against influenza A virus (A/California/07/09(H1N1)) pdm09 infected in MDCK cells assessed as decrease in virus titer by hemagglutination assay in presence of 1% suspension of chicken erythrocytes, CD50=47.5μM. | 25801933 | |||
| MDCK | Antiviral assay | 15 mins | Antiviral activity against Influenza A virus A/WSN/33(H1N1) infected in dog MDCK cells preincubated with virus for 15 mins followed by cells addition measured at 36 hrs post infection, IC50=39.6μM. | 26841168 | ||
| Raji | Antiviral assay | Antiviral activity against EBV infected in human Raji cells assessed as reduction in viral genome copy numbers by qRT-PCR analysis, EC50=30μM. | 30731401 | |||
| Vero E6 | Antiviral assay | 96 hrs | Antiviral activity against DENV2 16681 infected in African green monkey Vero E6 cells assessed as inhibitory rate of NS4B positive cells measured after 96 hrs incubation by DAPI staining based immunofluorescence method, IC50=8.1μM. | 31519375 | ||
| Vero E6 | Antiviral assay | 10 uM | 96 hrs | Antiviral activity against DENV2 16681 infected in African green monkey Vero E6 cells assessed as reduction in virus induced cytopathic effect at 10 uM measured after 96 hrs by reverse phase contrast microscopy | 31519375 | |
| RAW264.7 | Anti-inflammatory assay | 40 uM | 2 hrs | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production at 40 uM preincubated for 2 hrs followed by LPS addition measured after 20 hrs by Griess assay relative to control | ChEMBL | |
| RAW264.7 | Anti-inflammatory assay | 10 to 40 uM | 2 hrs | Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 10 to 40 uM preincubated for 2 hrs followed by LPS addition measured after 20 hrs by ELISA | ChEMBL | |
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| Molekulargewicht | 822.93 | Formel | C42H62O16 |
Lagerung (Ab dem Eingangsdatum) | |
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| CAS-Nr. | 1405-86-3 | SDF herunterladen | Lagerung von Stammlösungen |
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In vitro |
DMSO
: 100 mg/mL
(121.51 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.
| Targets/IC50/Ki |
11 beta-hydroxysteroid dehydrogenase
HMGB1
MAO
(Cell-free) 0.16 μM
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| In vitro |
Glycyrrhizin hemmt die Monoaminoxidase (MAO) mit einem IC50-Wert von 0,16 μM. |
| In vivo |
Glycyrrhizin erhöht die Spiegel von Monoaminen wie Adrenalin und Dopamin im Gehirn von Mäusen. |
Literatur |
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