nur für Forschungszwecke
Kat.-Nr.: S2404
Chemische Struktur
| Verwandte Ziele | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
|---|---|
| Weitere Aldose Reductase Inhibitoren | Epalrestat Obtusifolin Alrestatin Calceolarioside B Poliumoside Govorestat Soyasaponin Bb |
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | PMID |
|---|---|---|---|---|---|---|
| KB cells | Growth inhibition assay | Compound concentration required to reduce the exponential growth of KB cells by 50%, CC50=12 μM | ||||
| MT-4 cells | Growth inhibition assay | Compound concentration required to reduce the exponential growth of MT-4 cells by 50%, CC50=7.4 μM | ||||
| Hepa lclc7 cells | Cytotoxicity assay | Cytotoxicity against mouse Hepa lclc7 cells, IC50=39 μM | ||||
| J774.1 cells | Function assay | 24 h | Inhibition of LPS-induced NO production in mouse J774.1 cells after 24 hrs by Griess reagent assay, IC50=29.3 μM | |||
| colon 26-L5 cells | Cytotoxicity assay | 72 h | Cytotoxicity against mouse colon 26-L5 cells after 72 hrs by MTT assay, IC50=21.8 μM | |||
| MCF7 cells | Cytotoxicity assay | 25-150 μM | 72 h | Cytotoxicity against human MCF7 cells at 25 to 150 uM after 72 hrs by MTT assay | ||
| CHO cells | Cytotoxicity assay | Cytotoxicity against CHO cells by MTT assay, IC50=45.9 μM | ||||
| human T47D cells | Function assay | 96 h | Estrogenic activity in human T47D cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol after 96 hrs by alamar blue assay | |||
| MCF7 cells | Function assay | 96 h | Estrogenic activity in human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol after 96 hrs by alamar blue assay | |||
| MCF7 cells | Function assay | Estrogenic activity in luciferase transfected human MCF7 cells assessed as drug level causing stimulation of cell proliferation equivalent to 10 pM estradiol by luciferase reporter gene assay | ||||
| mouse NIH3T3 cells | Function assay | 8 h | Inhibition of cobalt chloride-induced HIF-1 activation expressed in mouse NIH3T3 cells after 8 hrs by luciferase reporter gene assay, IC50=4.8 μM | |||
| OE21 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human OE21 cells after 72 hrs by MTT assay, IC50=48 μM | |||
| U937 cells | Function assay | 5 ug/ml | 24 h | Antiinflammatory activity in human U937 cells assessed as inhibition of LPS-induced CCL5 secretion at 5 ug/ml after 24 hrs by ELISA relative to control | ||
| dog MDCK cells | Function assay | 20 ug/mL | 1 h | Antiviral activity against Influenza virus A/Puerto Rico/8/34 H1N1 infected in dog MDCK cells assessed as inhibition of viral replication at 20 ug/mL incubated at 1 hr post-infection measured after 24 hrs by hemagglutininating unit assay relative to control | ||
| dog MDCK cells | Function assay | 8 h | Inhibition of PKC/p38MAPK-mediated nuclear-cytoplasmic viral ribonucleoprotein export in dog MDCK cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 8 hrs post-infection by inmmunofluorescence | |||
| NCI-H292 cells | Function assay | Inhibition of PKC-mediated PKD phosphorylation in human NCI-H292 cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 6 hrs post-infection by immunoblotting analysis | ||||
| NCI-H292 cells | Function assay | Inhibition of PKC-mediated p38MAPK phosphorylation in human NCI-H292 cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 6 hrs post-infection by immunoblotting analysis | ||||
| NCI-H292 cells | Function assay | Inhibition of PKC-mediated JNK phosphorylation in human NCI-H292 cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 6 hrs post-infection by immunoblotting analysis | ||||
| dog MDCK cells | Function assay | Restoration of GSH level in dog MDCK cells infected with Influenza virus A/Puerto Rico/8/34 H1N1 measured at 24 hrs post-infection by DTNB-based colometric assay | ||||
| RBL-1 cells | Function assay | In vitro inhibition against 5-lipoxygenase in RBL-1 cells was determined, IC50=35 μM | ||||
| PC3 cells | Cytotoxicity assay | Cytotoxicity against human PC3 cells, IC50=46.4 μM | ||||
| HUVEC | Cytotoxicity assay | 48 h | Toxicity against HUVEC incubated for 48 hrs by MTT assay, IC50=41.17 μM | |||
| K562 cells | Cytotoxicity assay | 48 h | Antitumor activity against human K562 cells incubated for 48 hrs by MTT assay, IC50=29.27 μM | |||
| Hepa-1c1c7 cells | Function assay | Induction of quinone reductase activity in mouse Hepa-1c1c7 cells assessed as drug level required to double enzyme activity | ||||
| Hepa lclc7 cells | Function assay | Induction of mouse quinone reductase in mouse Hepa lclc7 cells assessed as concentration required to double enzyme activity | ||||
| U937 cells | Function assay | 5 ug/ml | Inhibition of LPS-induced AP-1 activation in human U937 cells at 5 ug/ml after 1 hr relative to control | |||
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
| Molekulargewicht | 256.25 | Formel | C15H12O4 |
Lagerung (Ab dem Eingangsdatum) | |
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| CAS-Nr. | 961-29-5 | SDF herunterladen | Lagerung von Stammlösungen |
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| Synonyme | N/A | Smiles | C1=CC(=CC=C1C=CC(=O)C2=C(C=C(C=C2)O)O)O | ||
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In vitro |
Ethanol : 26 mg/mL
DMSO
: 12 mg/mL
(46.82 mM)
Water : 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 |
Aldose reductase
(Cell-free assay) 320 nM
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| In vitro |
Isoliquiritigenin may be effective in preventing diabetic complications through inhibiting rat lens aldose reductase with an IC50 of 320 nM and sorbitol accumulation in human red blood cells with an IC50 of 2.0 μM. This compound may also serve as a skin-lightening agent by inhibiting mono- and diphenolase tyrosinase activities with an IC50 of 8.1 μM. It induces cell cycle arrest and cell growth inhibition in DU145 and LNCaP prostate cancer cell lines. This chemical induces apoptosis of human gastric cancer MGC-803 cells through increasing the intracellular free calcium concentration and decreasing the mitochondrial transmembrane potential (Deltapsi(m)).
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| In vivo |
LD50: Mice >6g/kg (i.g.)
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Literatur |
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