Name: Luteolin
Brand: Selleck Chemicals
SKU: S2320
Rating: 5 (29 reviews)

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Batch: Zuiverheid: 99.71%

99.71

Gerelateerde doelwitten	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Overig ADC Cytotoxin Inhibitoren	Triptolide SN-38 (+)-Bicuculline Rutin Artemisinin BHQ Pinocembrin Harmine hydrochloride Luteoloside Sacituzumab-govitecan

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving
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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	286.24	Formule	C₁₅H₁₀O₆	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	491-70-3	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel

Oplosbaarheid

In vitro
Batch:

DMSO : 33 mg/mL (115.28 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.850mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 57 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.350mg/ml (1.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 7 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

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.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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.

Werkingsmechanisme

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 is een flavonoïde die voorkomt in Terminalia chebula en die een niet-selectieve phosphodiesterase PDE-remmer is voor PDE1-5 met Ki-waarden van respectievelijk 15,0 μM, 6,4 μM, 13,9 μM, 11,1 μM en 9,5 μM. Deze verbinding remt de LPS-gestimuleerde TNF-alfa-productie met een IC50 van minder dan 1 μM. Het remt de LPS-geïnduceerde fosforylering van Akt en van IkappaBalpha.
In vivo	LD50: Muizen >2500mg/kg (i.g.)
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/19853596/ [2] https://pubmed.ncbi.nlm.nih.gov/11123379/

Toepassingen

Methoden	Biomarkers	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