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Cat.nr.: S2314
| Gerelateerde doelwitten | Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR PGES |
|---|---|
| Overig Estrogen/progestogen Receptor Inhibitoren | Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV-471) MPP dihydrochloride Cholesterol PHTPP G15 Licochalcone A Endoxifen HCl Pregnenolone Chrysin |
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| HEK293 FS cells | Function assay | Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=1.2 μM | ||||
| human HeLa cells | Function assay | Inhibition of MRP1 transfected in human HeLa cells assessed as inhibition of [3H]LTC4 transport by rapid filtration assay, Ki=2.4 μM | ||||
| human MV4-11 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human MV4-11 cells harboring FLT3 mutation after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=3.34 μM | |||
| MDCK cells | Function assay | Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=4.7 μM | ||||
| human MDA-kb2 cells | Function assay | Antagonist activity at androgen receptor in human MDA-kb2 cells assessed as inhibition of DHT-induced luciferase activity by luciferase reporter gene assay, IC50=9.7 μM | ||||
| B16-4A5 cells | Function assay | Inhibition of melanogenesis in theophylline-stimulated mouse B16-4A5 cells after 72 hrs, IC50=20 μM | ||||
| human HL60 cells | Cytotoxicity assay | Cytotoxicity against human HL60 cells assessed as cell survival at 50 uM after 72 hrs by CCK8 assay | ||||
| mouse 3T3L1 cells | Function assay | Inhibition of AMPK-mediated adipocyte differentiation in mouse 3T3L1 cells | ||||
| mouse RAW264.7 cells | Function assay | Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 1 to 100 uM after 24 hrs by Griess method | ||||
| mouse L929 cells | Function assay | Inhibition of recombinant human TNF-alpha-induced cytotoxicity of mouse L929 cells assessed as survivality treated with drug after 2 hrs of TNFalpha treatment | ||||
| human U87 cells | Cytotoxicity assay | 5-40 μM | 72 h | Cytotoxicity against human U87 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | ||
| human A549 cells | Cytotoxicity assay | 5-40 μM | 72 h | Cytotoxicity against human A549 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | ||
| human MCF7 cells | Cytotoxicity assay | 5-40 μM | 72 h | Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | ||
| MDA-MB-231 cells | Cytotoxicity assay | 5-40 μM | 72 h | Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | ||
| MDCK cells | Function assay | 50 μM | Antiviral activity against influenza A virus H1N1 A/PR/8/34 infected in MDCK cells assessed as reduction in fluorescence positive cells at 50 uM immunofluorescence assay | |||
| human NCI-H2126 cells | Cytotoxicity assay | 5-40 μM | 72 h | Cytotoxicity against human NCI-H2126 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | ||
| human SMMC7721 cells | Cytotoxicity assay | 5-40 μM | 72 h | Cytotoxicity against human SMMC7721 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | ||
| human PANC1 cells | Cytotoxicity assay | 5-40 μM | 72 h | Cytotoxicity against human PANC1 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | ||
| human BxPC3 cells | Cytotoxicity assay | 5-40 μM | 72 h | Cytotoxicity against human BxPC3 cells assessed as reduction in cell viability at 5 to 40 uM after 72 hrs by MTT assay | ||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
| Molecuulgewicht | 286.23 | Formule | C15H10O6 |
Opslag (vanaf de datum van ontvangst) | |
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| CAS-nr. | 520-18-3 | SDF downloaden | Opslag van stamoplossingen |
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In vitro |
Ethanol : 28 mg/mL
DMSO
: 27 mg/mL
(94.32 mM)
Water : Insoluble |
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In vivo |
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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 |
ERRα
ERRγ
Topo I
fatty acid synthase
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Referenties |
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(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Werving | Aandoeningen | Sponsor/medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| NCT05073523 | Completed | Healthy |
Chalmers University of Technology |
September 27 2021 | Not Applicable |