alleen voor onderzoeksdoeleinden
Cat.nr.: S2302
Chemische structuur
| Gerelateerde doelwitten | HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase |
|---|---|
| Overig Dehydrogenase Inhibitoren | Vorasidenib (AG-881) (R)-GNE-140 CPI-613 (Devimistat) Sodium Dichloroacetate (DCA) AGI-6780 Gossypol Acetate Emodin AGI-5198 Brequinar (DUP785) NCT-503 |
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | 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 | |
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
| Molecuulgewicht | 822.93 | Formule | C42H62O16 |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 1405-86-3 | SDF downloaden | Opslag van stamoplossingen |
|
|
|
In vitro |
DMSO
: 100 mg/mL
(121.51 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.
Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
| Targets/IC50/Ki |
11 beta-hydroxysteroid dehydrogenase
HMGB1
MAO
(Cell-free) 0.16 μM
|
|---|---|
| In vitro |
Glycyrrhizin inhibits monoamine oxidase (MAO) with the IC50 value of 0.16 μM. |
| In vivo |
Glycyrrhizin increases the levels of monoamines like epinephrine and dopamine in brains of mice. |
Referenties |
|