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N. Cat.S2302
| Target correlati | HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite |
|---|---|
| Altro Dehydrogenase Inibitori | Vorasidenib (AG-881) (R)-GNE-140 CPI-613 (Devimistat) Sodium Dichloroacetate (DCA) AGI-5198 Gossypol Acetate AGI-6780 Emodin NCT-503 Brequinar |
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | 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 | |
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 822.93 | Formula | C42H62O16 |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 1405-86-3 | Scarica SDF | Conservazione delle soluzioni stock |
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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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Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.
| Targets/IC50/Ki |
11 beta-hydroxysteroid dehydrogenase
HMGB1
MAO
(Cell-free) 0.16 μM
|
|---|---|
| In vitro |
La glicirrizina inibisce la monoaminossidasi (MAO) con un valore di IC50 di 0,16 μM. |
| In vivo |
La glicirrizina aumenta i livelli di monoamine come l'epinefrina e la dopamina nel cervello dei topi. |
Riferimenti |
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Istruzioni per la manipolazione
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