endast för forskning
Kat.nr.: S2320
Kemisk struktur
| Relaterade mål | Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism |
|---|---|
| Övrigt ADC Cytotoxin Inhibitorer | Triptolide SN-38 (+)-Bicuculline Rutin Artemisinin BHQ Pinocembrin Luteoloside Lappaconite HBr Gramine |
| Cellinjer | Analystyp | Koncentration | Inkubationstid | Formulering | Aktivitetsbeskrivning | 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 | ||
| Klicka för att visa mer experimentella data för cellinjer | ||||||
| Molekylvikt | 286.24 | Formel | C15H10O6 |
Lagring (från mottagningsdatumet) | |
|---|---|---|---|---|---|
| CAS-nr | 491-70-3 | Ladda ner SDF | Lagring av stamlösningar |
|
|
|
In vitro |
DMSO
: 33 mg/mL
(115.28 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)
Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)
Beräkningsresultat:
Arbetskoncentration: mg/ml;
Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )
Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH2O, blanda och klarna.
Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.
Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.
| 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 a flavonoid found in Terminalia chebula, which is a non-selective phisphodiesterase PDE inhibitor for PDE1-5 with Ki of 15.0 μM, 6.4 μM, 13.9 μM, 11.1 μM and 9.5 μM, respectively. This compound inhibits LPS-stimulated TNF-alpha production with an IC50 of less than 1 μM. It inhibites LPS-induced phosphorylation of Akt as well as IkappaBalpha. |
| In vivo |
LD50: Mice >2500mg/kg (i.g.) |
Referenser |
|
| Metoder | Biomarkörer | Bilder | 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 |
Fråga 1:
Would you please suggest a suitable vehicle to dissolve it for in vivo i.p. use?
Svar:
Formula: 5% DMSO+40% PEG 300+5% Tween80+ddH2O, working Solution concentration: up to 7.5mg/ml, stable for 30min.