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Réf. CatalogueS2314
| Cibles apparentées | Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR |
|---|---|
| Autre Estrogen/progestogen Receptor Inhibiteurs | Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV-471) MPP dihydrochloride Cholesterol G15 Endoxifen HCl Licochalcone A Chrysin Pregnenolone AZD9496 |
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | 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 | ||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 286.23 | Formule | C15H10O6 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 520-18-3 | Télécharger le SDF | Stockage des solutions mères |
|
|
|
In vitro |
Ethanol : 28 mg/mL
DMSO
: 27 mg/mL
(94.32 mM)
Water : Insoluble |
|
In vivo |
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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
| Targets/IC50/Ki |
ERRα
ERRγ
Topo I
fatty acid synthase
|
Références |
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(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| NCT05073523 | Completed | Healthy |
Chalmers University of Technology |
September 27 2021 | Not Applicable |
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