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Réf. Catalogue: S2320
| Cibles apparentées | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
|---|---|
| Autre ADC Cytotoxin Inhibiteurs | Triptolide SN-38 (+)-Bicuculline Rutin Artemisinin BHQ Pinocembrin Luteoloside Lappaconite HBr Gramine |
| Lignées cellulaires | Type d'essai | Concentration | Temps d'incubation | Formulation | Description de l'activité | PMID |
|---|---|---|---|---|---|---|
| mouse RAW264.7 cells | Function assay | 2 h | Inhibition of NO production in LPS-stimulated mouse RAW264.7 cells pre-incubated for 2 hrs before LPS stimulation for 24 hrs by Griess assay method, IC50=0.21 μM | |||
| HEK293 FS cells | Function assay | Inhibition of NOX4 expressed in HEK293 FS cells assessed as H2O2 production by H2O2/Tyr/LPO assay, IC50=0.85 μM | ||||
| CHO cells | Function assay | Agonist activity at rat DAT expressed in CHO cells, EC50=1.45 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=1.76 μM | |||
| HEK293 cells | Function assay | 24 h | Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay, EC50=2.3 μM | |||
| human U2OS cells | Function assay | 5 h | Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay, EC50=3.2 μM | |||
| RBL-2H3 cells | Function assay | Inhibitory activity against IL-4 production in RBL-2H3 cells was determined, IC50=3.7 μM | ||||
| human mast cells | Function assay | Inhibition of SYK in human mast cells assessed as reduction in mast cell degranulation, EC50=4.5 μM | ||||
| human LNCAP cells | Function assay | Downregulation of prostate specific antigen secretion in human LNCAP cells, IC50=5 μM | ||||
| rat H9c2 cells | Function assay | 24 h | Cytoprotective activity against doxorubicin-induced cytotoxicity in rat H9c2 cells assessed as cell viability after 24 hrs by MTT assay, EC50=5.53 μM | |||
| human HT-29 cells | Function assay | 10 mins | Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay, EC50=7.24 μM | |||
| human RS4:11 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human RS4:11 cells harboring wild type FLT3 after 72 hrs by tetrazolium based Ez CyTox cell viability assay, GI50=7.25 μM | |||
| NCI-H460 cells | Function assay | 2-20 h | Inhibition of ABCG2 expressed in human NCI-H460 cells assessed as inhibition of PhA accumulation after 2 to 20 hrs relative to fumitremorgin C, IC50=8.9 μM | |||
| human H9 cells | Function assay | 3 days | Antiviral activity against HIV1 3B infected in human H9 cells assessed as inhibition of viral replication after 3 days by p24 antigen capture assay, EC50=10 μM | |||
| MDCK cells | Cytotoxicity assay | Cytotoxicity against MDCK cells by MTT assay, CC50=12.44 μM | ||||
| mouse B16-4A5 cells | Function assay | 72 h | Inhibition of theophylline-stimulated melanogenesis in mouse B16-4A5 cells after 72 hrs, IC50=14 μM | |||
| K562 cells | Growth inhibition assay | 5 days | Growth inhibition of K562 cells by XTT assay after 5 days, IC50=14.65 μM | |||
| human H9 cells | Cytotoxicity assay | 3 days | Cytotoxicity against human H9 cells after 3 days, IC50=16 μM | |||
| human HT-29 cells | Function assay | 10 mins | Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins, IC50=18.6 μM | |||
| human U937 cells | Proliferation assay | 72 h | Antiproliferative activity against human U937 cells after 72 hrs by WST-8 assay, IC50=20 μM | |||
| mouse HT22 cells | Function assay | 3 h | Neuroprotective activity in mouse HT22 cells assessed as t-BOOH-induced toxicity at 40 uM preincubated for 3 hrs followed by t-BOOH induction measured after 9 hrs by MTT assay | |||
| human THP1 cells | Function assay | 20 μM | 1 h | Downregulation of TPA-induced NOX2 mRNA expression in human THP1 cells at 20 uM incubated for 1 hr prior to TPA challenge measured after 24 hrs by RT-PCR analysis | ||
| MDA-MB-231 cells | Function assay | 5 μM | 16 h | Inhibition of PMA-stimulated NF-kappaB signaling (unknown origin) expressed in MDA-MB-231 cells at 5 uM incubated for 16 hrs by luciferase reporter gene assay | ||
| HL60 cells | Proliferation assay | 30 μM | 48 h | Antiproliferative activity against human HL60 cells at 30 uM after 48 hrs by MTS assay | ||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 286.24 | Formule | C15H10O6 |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 491-70-3 | Télécharger le SDF | Stockage des solutions mères |
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In vitro |
DMSO
: 33 mg/mL
(115.28 mM)
Water : Insoluble Ethanol : Insoluble |
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In vivo |
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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y 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 d'abord 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 d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout 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 |
PDE2
(Cell-free assay) 6.4 μM(Ki)
PDE5
(Cell-free assay) 9.5 μM(Ki)
PDE4
(Cell-free assay) 11.1 μM(Ki)
PDE3
(Cell-free assay) 13.9 μM(Ki)
PDE1
(Cell-free assay) 15.0 μM(Ki)
|
|---|---|
| In vitro |
Luteolin est un flavonoïde trouvé dans Terminalia chebula, qui est un inhibiteur non sélectif de la phosphodiesterase PDE pour PDE1-5 avec un Ki de 15,0 μM, 6,4 μM, 13,9 μM, 11,1 μM et 9,5 μM, respectivement. Ce composé inhibe la production de TNF-alpha stimulée par le LPS avec une IC50 inférieure à 1 μM. Il inhibe la phosphorylation d'Akt ainsi que d'IkappaBalpha induite par le LPS. |
| In vivo |
DL50: Souris >2500mg/kg (i.g.) |
Références |
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| Méthodes | Biomarqueurs | Images | PMID |
|---|---|---|---|
| Western blot | FADD / PARP / Cleaved PARP Caspase-3 / Cleaved Caspase-3 / Caspase-8 / Cleaved Caspase-8 ERK / p-ERK / JNK / p-JNK / p38 / p-p38 / Bax / Bcl-2 p-VEGFR2 / p-mTOR / pS6K1 / p70S6K1 / pAKT / AKT / MMP-2 / MMP-9 p21 / Survivin / Cyclin D1 DNMT1 / DMNT3A / DNMT3B TET1 / TET2 / TET3 |
|
30992674 |
| Immunofluorescence | 5-hmC |
|
30988303 |
| Growth inhibition assay | Cell viability |
|
30992674 |
Question 1:
Would you please suggest a suitable vehicle to dissolve it for in vivo i.p. use?
Réponse :
Formula: 5% DMSO+40% PEG 300+5% Tween80+ddH2O, working Solution concentration: up to 7.5mg/ml, stable for 30min.