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Glycyrrhizin (Glycyrrhizic Acid, NSC 167409) HMGB1-remmer

Cat.Nr.: S2302

Glycyrrhizin (NSC 167409, Glycyrrhizic Acid) is een directe HMGB1 (high mobility group box 1) remmer die HMGB1-afhankelijke ontsteking molecule expressie en oxidatieve stress remt; moduleert P38 en P-JNK maar niet p-ERK signalering; Remt ook 11 beta-hydroxysteroid dehydrogenase en monoamine oxidase (MAO).
Glycyrrhizin (Glycyrrhizic Acid, NSC 167409) Dehydrogenase Remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 822.93

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.73%
99.73

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

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
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Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht 822.93 Formule

C42H62O16

Opslag (Vanaf de ontvangstdatum)
CAS-nr. 1405-86-3 SDF downloaden Opslag van stamoplossingen

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (121.51 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa Concentratie Volume Moleculair gewicht
Verdunningscalculator Moleculair gewicht calculator

In vivo
Batch:

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

mg/kg g μL

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 het gedeelte Oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH2O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

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. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC50/Ki
11 beta-hydroxysteroid dehydrogenase
HMGB1
MAO
(Cell-free)
0.16 μM
In vitro

Glycyrrhizin remt monoamine oxidase (MAO) met een IC50-waarde van 0,16 μM.

In vivo

Glycyrrhizin verhoogt de niveaus van monoamines zoals epinefrine en dopamine in de hersenen van muizen.

Referenties
  • [4] https://pubmed.ncbi.nlm.nih.gov/1913999/