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N. Cat.S2314
| Target correlati | Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR |
|---|---|
| Altro Estrogen/progestogen Receptor Inibitori | Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV-471) MPP dihydrochloride Cholesterol G15 Endoxifen HCl Licochalcone A Chrysin Pregnenolone AZD9496 |
| Linee cellulari | Tipo di saggio | Concentrazione | Tempo di incubazione | Formulazione | Descrizione dellattività | 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 | ||
| Clicca per visualizzare più dati sperimentali sulle linee cellulari | ||||||
| Peso molecolare | 286.23 | Formula | C15H10O6 |
Conservazione (Dalla data di ricezione) | |
|---|---|---|---|---|---|
| N. CAS | 520-18-3 | Scarica SDF | Conservazione delle soluzioni stock |
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In vitro |
Ethanol : 28 mg/mL
DMSO
: 27 mg/mL
(94.32 mM)
Water : Insoluble |
|
In vivo |
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Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)
Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)
Risultati del calcolo:
Concentrazione di lavoro: mg/ml;
Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.
Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.
Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.
| Targets/IC50/Ki |
ERRα
ERRγ
Topo I
fatty acid synthase
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Riferimenti |
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(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)
| Numero NCT | Reclutamento | Condizioni | Sponsor/Collaboratori | Data di inizio | Fasi |
|---|---|---|---|---|---|
| NCT05073523 | Completed | Healthy |
Chalmers University of Technology |
September 27 2021 | Not Applicable |
Istruzioni per la manipolazione
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