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Réf. CatalogueS2302
| Cibles apparentées | HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite |
|---|---|
| Autre Dehydrogenase Inhibiteurs | Vorasidenib (AG-881) (R)-GNE-140 CPI-613 (Devimistat) Sodium Dichloroacetate (DCA) AGI-5198 Gossypol Acetate AGI-6780 Emodin NCT-503 Brequinar |
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | 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 | |
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 822.93 | Formule | C42H62O16 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 1405-86-3 | Télécharger le SDF | Stockage des solutions mères |
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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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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
| Targets/IC50/Ki |
11 beta-hydroxysteroid dehydrogenase
HMGB1
MAO
(Cell-free) 0.16 μM
|
|---|---|
| In vitro |
La glycyrrhizine inhibe la monoamine oxydase (MAO) avec une valeur IC50 de 0,16 μM. |
| In vivo |
La glycyrrhizine augmente les niveaux de monoamines comme l'épinéphrine et la dopamine dans le cerveau des souris. |
Références |
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