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Cat.nr.: S1696
Chemische structuur
| Gerelateerde doelwitten | Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR PGES |
|---|---|
| Overig Glucocorticoid Receptor Inhibitoren | Relacorilant (CORT125134) Corticosterone AL082D06 (20S)-Protopanaxatriol Cortodoxone |
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| mouse RAW264.7 cells | Function assay | 24 h | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction, IC50=0.061 μM | 21361338 | ||
| mouse L929 cells | Growth inhibition assay | 6 days | Growth inhibition of mouse L929 cells after 6 days | 926113 | ||
| RAW264.7 | Antiinflammatory assay | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production by MTT assay, IC50 = 40.64 μM. | 20879743 | |||
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess reaction based spectrophotometry, IC50 = 40.64 μM. | 21807513 | ||
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess reaction, IC50 = 40.64 μM. | 23067550 | ||
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 43.8 μM. | 23755850 | ||
| L929 | Function assay | 20 hrs | Displacement of 1 x 10'-8 M of [1,2,3-3H]-triamcinolone acetonide from glucocorticoid receptor in soluble fraction of mouse L929 cells after 20 hrs, Kd = 0.043 μM. | 926113 | ||
| HEK293 | Function assay | Inhibition of MR-mediated transactivation of galactosidase reporter gene in HEK293 cells expressing 11betaHSD1 | 16759088 | |||
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of IL-10 production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by ELISA relative to control | 21384845 | |
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of IL-6 production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by ELISA relative to control | 21384845 | |
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of IL1-beta production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by ELISA relative to control | 21384845 | |
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of TNFalpha production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by ELISA relative to control | 21384845 | |
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by Griess reaction method relative to control | 21384845 | |
| neural precursor cells | Function assay | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 17417631 | |||
| RAW264.7 | Antiinflammatory assay | 10 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced increase in TNF-alpha level at 10 uM incubated for 2 hrs prior to LPS challenge measured after 22 hrs by ELISA relative to control | 25515561 | |
| RAW264.7 | Antiinflammatory assay | 10 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced increase in IL-6 level at 10 uM incubated for 2 hrs prior to LPS challenge measured after 22 hrs by ELISA relative to control | 25515561 | |
| RAW264.7 | Antiinflammatory assay | 10 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced increase in IL-1beta level at 10 uM incubated for 2 hrs prior to LPS challenge measured after 22 hrs by ELISA relative to control | 25515561 | |
| RAW264.7 | Antiinflammatory assay | 10 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 10 uM incubated for 2 hrs prior to LPS challenge measured after 22 hrs relative to vehicle-treated control | 25515561 | |
| B16F10 | Apoptosis assay | 20 uM | 36 hrs | Induction of apoptosis in mouse B16F10 cells assessed as increase in cleaved caspase 3 level at 20 uM after 36 hrs by western blot analysis | 26695732 | |
| B16F10 | Apoptosis assay | 20 uM | 36 hrs | Induction of apoptosis in mouse B16F10 cells assessed as increase in p53 expression at 20 uM after 36 hrs by propidium iodide staining based FACS analysis | 26695732 | |
| B16F10 | Apoptosis assay | 20 uM | 36 hrs | Induction of apoptosis in mouse B16F10 cells assessed as increased Bax expression at 20 uM after 36 hrs by western blot analysis | 26695732 | |
| B16F10 | Antitumor activity assay | 6.11 mg/kg | Antitumor activity against mouse B16F10 cells xenografted in C57BL/J mouse assessed as inhibition of tumor growth at 6.11 mg/kg, ip | 26695732 | ||
| B16F10 | Apoptosis assay | 20 uM | 36 hrs | Induction of apoptosis in mouse B16F10 cells assessed as increase in cytochrome C level at 20 uM after 36 hrs by western blot analysis | 26695732 | |
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
| Molecuulgewicht | 362.46 | Formule | C21H30O5 |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 50-23-7 | SDF downloaden | Opslag van stamoplossingen |
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| Synoniemen | NSC 10483 | Smiles | CC12CCC(=O)C=C1CCC3C2C(CC4(C3CCC4(C(=O)CO)O)C)O | ||
|
In vitro |
DMSO
: 72 mg/mL
(198.64 mM)
Ethanol : 15 mg/mL Water : Insoluble |
|
In vivo |
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Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
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.)
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.
| Targets/IC50/Ki |
Glucocorticoid receptor
|
|---|---|
| In vitro |
Hydrocortisone prevents endothelial barrier breakdown in response to pro-inflammatory stimuli (TNFalpha administration) in the human brain microvascular endothelial cell line hCMEC/D3, which could be demonstrated to be partly based on maintenance of occludin levels. This compound-treated dendritic cells (DCs) show a decreased expression of MHC II molecules, the costimulatory molecule CD86, and the DC-specific marker CD83, as well as a strongly reduced IL-12 secretion. It inhibits production of IFN-gamma but induces an increased release of IL-4 and no change in IL-5. This chemical reduces T-cell proliferation in dendritic cells. It prevents TNF-alpha induced severe degradation of the glycocalyx, increased coronary resistance, heightened vascular leak and permeability to hydroxyethyl starch and caused mast-cell degranulation in isolated guinea pig hearts. This compound reduces postischemic oxidative stress, perfusion pressure, and transudate formation in isolated guinea pig hearts. It inhibits postischemic shedding of syndecan-1, heparan sulfate, and hyaluronan, as well as release of histamine from resident mast cells. It increases the levels of IL-4-induced germ line C epsilon transcripts by twofold and delivers the signal required for transcription of mature C epsilon mRNA. This chemical induces S mu-S epsilon deletional switch recombination in IL-4-treated B cells, and support a model of sequential isotype switching from IgM to IgE via IgG4. |
Referenties |
|
| Methoden | Biomarkers | Afbeeldingen | PMID |
|---|---|---|---|
| Western blot | parkin / AIMP2 CREB |
|
28366931 |
| Immunofluorescence | Glut2 |
|
29717618 |
| Growth inhibition assay | Cell viability |
|
22829975 |
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Werving | Aandoeningen | Sponsor/medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| NCT05741762 | Active not recruiting | Critical Illness|Adrenal Insufficiency|Septic Shock |
Dr Adnan Agha|United Arab Emirates University |
January 31 2023 | -- |
| NCT05607901 | Recruiting | Dermatologic Disease |
Tanta University |
October 28 2022 | Phase 2 |
| NCT05324618 | Completed | Atopic|Dermatitis |
Ain Shams University|National Hepatology & Tropical Medicine Research Institute |
May 15 2022 | Phase 4 |